Roush, William

Faculty Member Emeritus

Positions

2018 - Professor Emeritus, Chemistry , Scripps Research
2004 - Associate Dean, Skaggs Graduate School of Chemical and Biological Sciences , Scripps Research
2004 - Faculty Member, Skaggs Graduate School of Chemical and Biological Sciences , Scripps Research
2004 - 2018 Professor, Chemistry , Scripps Research
1997 - 2005 Warner Lambert/Parke-Davis Professor of Chemistry, University of Michigan
2002 - 2004 Chair, Department of Chemistry, University of Michigan
1995 - 1997 Distinguished Professor of Chemistry, Indiana University
1989 - 1995 Professor of Chemistry, Indiana University
1987 - 1989 Associate Professor of Chemistry, Indiana University
1983 - 1986 Associate Professor of Chemistry, Massachusetts Institute of Technology
1978 - 1983 Assistant Professor of Chemistry, Massachusetts Institute of Technology
1977 - 1978 Postdoctoral Fellow, Harvard University

Dr. William Roush focuses on the total synthesis of structurally complex and biologically interesting natural products, development of new synthetic methods and strategies, and on problems in medicinal and bioorganic chemistry.

Contact

roush@scripps.edu

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recent publications

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academic article
- Nilchan, N., Alburger, J. M., Roush, W. R., Rader, C. An Engineered Arginine Residue of Unusual pH-Sensitive Reactivity Facilitates Site-Selective Antibody Conjugation Biochemistry 2021 60:1080-1087 DOI:10.1021/acs.biochem.0c00955 PMID:33754696
- Lo, C. H., Shay, G., McGuire, J. J., Li, T., Shain, K. H., Choi, J. Y., Fuerst, R., Roush, W. R., Knapinska, A. M., Fields, G. B., Lynch, C. C. Host-Derived Matrix Metalloproteinase-13 Activity Promotes Multiple Myeloma-Induced Osteolysis and Reduces Overall Survival Cancer Research 2021 81:2415-2428 DOI:10.1158/0008-5472.Can-20-2705 PMID:33526510
- Jilkova, A., Rubesova, P., Fanfrlik, J., Fajtova, P., Rezacova, P., Brynda, J., Lepsik, M., Mertlikova-Kaiserova, H., Emal, C. D., Renslo, A. R., Roush, W. R., Horn, M., et al. Druggable Hot Spots in the Schistosomiasis Cathepsin B1 Target Identified by Functional and Binding Mode Analysis of Potent Vinyl Sulfone Inhibitors Acs Infectious Diseases 2020 7:1077-1088 DOI:10.1021/acsinfecdis.0c00501 PMID:33175511 PMCID:PMC8154419
- Vena, F., Bayle, S., Nieto, A., Quereda, V., Aceti, M., Frydman, S. M., Sansil, S. S., Grant, W., Monastyrskyi, A., McDonald, P., Roush, W. R., Teng, M. X., et al. Targeting Casein Kinase 1 Delta Sensitizes Pancreatic and Bladder Cancer Cells to Gemcitabine Treatment by Upregulating Deoxycytidine Kinase Molecular Cancer Therapeutics 2020 19:1623-1635 DOI:10.1158/1535-7163.Mct-19-0997 PMID:32430484 PMCID:PMC7415672
- Maharaj, K., Powers, J. J., Achille, A., Mediavilla-Varela, M., Gamal, W., Burger, K. L., Fonseca, R., Jiang, K., Miskin, H. P., Maryanski, D., Monastyrskyi, A., Duckett, D. R., et al. The dual PI3Kδ/CK1ε inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells Blood Advances 2020 4:3072-3084 DOI:10.1182/bloodadvances.2020001800 PMID:32634240 PMCID:PMC7362385
- Quereda, V., Bayle, S., Vena, F., Frydman, S. M., Monastyrskyi, A., Roush, W. R., Duckett, D. R. Therapeutic targeting of CDK12/CDK13 in triple-negative breast cancer Cancer Cell 2019 36:545-558 DOI:10.1016/j.ccell.2019.09.004 PMID:31668947
- Renner, K., Bruss, C., Schnell, A., Koehl, G., Becker, H. M., Fante, M., Menevse, A. N., Kauer, N., Blazquez, R., Hacker, L., Decking, S. M., Bohn, T., et al. Restricting glycolysis preserves T cell effector functions and augments checkpoint therapy Cell Reports 2019 29:135-150 DOI:10.1016/j.celrep.2019.08.068 PMID:31577944
- Hwang, D.*, Nilchan, N.*, Nanna, A. R., Li, X., Cameron, M. D., Roush, W. R., Park, H., Rader, C. Site-selective antibody functionalization via orthogonally reactive arginine and lysine residues Cell Chemical Biology 2019 26:1229-1239 DOI:10.1016/j.chembiol.2019.05.010 PMID:31231031 PMCID:PMC6754284 (* = equal contribution)
- Doebelin, C., He, Y., Campbell, S., Nuhant, P., Kumar, N., Koenig, M., Garcia-Ordonez, R., Chang, M. R., Roush, W. R., Lin, L., Kahn, S., Cameron, M. D., et al. Discovery and optimization of a series of sulfonamide inverse agonists for the retinoic acid receptor-related orphan receptor-α Medicinal Chemistry 2019 15:676-684 DOI:10.2174/1573406415666190222124745 PMID:30799793
- Fuerst, R., Yong Choi, J., Knapinska, A. M., Smith, L., Cameron, M. D., Ruiz, C., Fields, G. B., Roush, W. R. Development of matrix metalloproteinase-13 inhibitors - A structureactivity/structure-property relationship study Bioorganic & Medicinal Chemistry 2018 26:4984-4995 DOI:10.1016/j.bmc.2018.08.020 PMID:30249495
- Persi, E., Duran-Frigola, M., Damaghi, M., Roush, W. R., Aloy, P., Cleveland, J. L., Gillies, R. J., Ruppin, E. Systems analysis of intracellular pH vulnerabilities for cancer therapy Nature Communications 2018 9 DOI:10.1038/s41467-018-05261-x PMID:30065243 PMCID:PMC6068141
- Zyserman, I., Mondal, D., Sarabia, F., McKerrow, J. H., Roush, W. R., Debnath, A. Identification of cysteine protease inhibitors as new drug leads against Naegleria fowleri Experimental Parasitology 2018 188:36-41 DOI:10.1016/j.exppara.2018.03.010 PMID:29551628 PMCID:PMC5918159
- Monastyrskyi, A., Nilchan, N., Quereda, V., Noguchi, Y., Ruiz, C., Grant, W., Cameron, M., Duckett, D., Roush, W. Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer Bioorganic & Medicinal Chemistry 2018 26:590-602 DOI:10.1016/j.bmc.2017.12.020 PMID:29289448 PMCID:PMC5803353
- Monastyrskyi, A., Bayle, S., Quereda, V., Grant, W., Cameron, M., Duckett, D., Roush, W. Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors Bioorganic & Medicinal Chemistry Letters 2018 28:400-404 DOI:10.1016/j.bmcl.2017.12.026 PMID:29277458
- Wood, S. D., Grant, W., Adrados, I., Choi, J. Y., Alburger, J. M., Duckett, D. R., Roush, W. R. In silica HTS and structure based optimization of indazole-derived ULK1 inhibitors ACS Medicinal Chemistry Letters 2017 8:1258-1263 DOI:10.1021/acsmedchemlett.7b00344 PMID:29259744 PMCID:PMC5733266
- Rondini, E. A., Mladenovic-Lucas, L., Roush, W. R., Halvorsen, G. T., Green, A. E., Granneman, J. G. Novel pharmacological probes reveal ABHD5 as a locus of lipolysis control in white and brown adipocytess Journal of Pharmacology and Experimental Therapeutics 2017 363:367-376 DOI:10.1124/jpet.117.243253 PMID:28928121 PMCID:PMC5698943
- Nanna, A. R., Li, X., Walseng, E., Pedzisa, L., Goydel, R. S., Hymel, D., Burke, T. R., Roush, W. R., Rader, C. Harnessing a catalytic lysine residue for the one-step preparation of homogeneous antibody-drug conjugates Nature Communications 2017 8 DOI:10.1038/s41467-017-01257-1 PMID:29062027 PMCID:PMC5653646
- Choi, J. Y., Fuerst, R., Knapinska, A. M., Taylor, A. B., Smith, L., Cao, X., Hart, P. J., Fields, G. B., Roush, W. R. Structure-based design and synthesis of potent and selective matrix metalloproteinase 13 inhibitors Journal of Medicinal Chemistry 2017 60:5816-5825 DOI:10.1021/acs.jmedchem.7b00514 PMID:28653849
- Allais, C., Roush, W. R. Enantio- and diastereoselective synthesis of 1,5-syn-(Z)-amino alcohols via imine double allylboration: Synthesis of trans-1,2,3,6-tetrahydropyridines and total synthesis of andrachcine Organic Letters 2017 19:2646-2649 DOI:10.1021/acs.orglett.7b00995 PMID:28471668
- Bhowmick, M., Tokmina-Roszyk, D., Onwuha-Ekpete, L., Harmon, K., Robichaud, T., Fuerst, R., Stawikowska, R., Steffensen, B., Roush, W., Wong, H. R., Fields, G. B. Second generation triple-helical peptide inhibitors of matrix metalloproteinases Journal of Medicinal Chemistry 2017 60:3814-3827 DOI:10.1021/acs.jmedchem.7b00018 PMID:28394608
- Mason, J. W., Schmid, C. L., Bohn, L. M., Roush, W. R. Stolonidiol: Synthesis, target identification, and mechanism for choline acetyltransferase activation Journal of the American Chemical Society 2017 139:5865-5869 DOI:10.1021/jacs.7b01083 PMID:28414442
- Getun, I. V., Wu, Z., Fallahi, M., Ouizem, S., Liu, Q., Li, W., Costi, R., Roush, W. R., Cleveland, J. L., Bois, P. R. J. Functional roles of acetylated histone marks at mouse meiotic recombination hot spots Molecular and Cellular Biology 2017 37:UNSP e00942-15 DOI:10.1128/mcb.00942-15 PMID:27821479 PMCID:PMC5247613
- Calvet, C. M., Choi, J. Y., Thomas, D., Suzuki, B., Hirata, K., Lostracco-Johnson, S., de Mesquita, L. B., Nogueira, A., Meuser-Batista, M., Silva, T. A., Siqueira-Neto, J. L., Roush, W. R., et al. 4-aminopyridyl-based lead compounds targeting CYP51 prevent spontaneous parasite relapse in a chronic model and improve cardiac pathology in an acute model of Trypanosoma cruzi infection PLoS Neglected Tropical Diseases 2017 11 DOI:10.1371/journal.pntd.0006132 PMID:29281643 PMCID:PMC5744913
- Choi, J. Y., Roush, W. R. Structure Based Design of CYP51 Inhibitors Current Topics in Medicinal Chemistry 2017 17:30-39 DOI:10.2174/1568026616666160719164933 PMID:27449014
- Patterson, J. T., Wilson, H. D., Asano, S., Nilchan, N., Fuller, R. P., Roush, W. R., Rader, C., Barbas III, C. F. Human serum albumin domain I fusion protein for antibody conjugation Bioconjugate Chemistry 2016 27:2271-2275 DOI:10.1021/acs.bioconjchem.6b00432 PMID:27666414
- Walseng, E., Nelson, C. G., Qi, J., Nanna, A. R., Roush, W. R., Goswami, R. K., Sinha, S. C., Burke Jr., T. R., Rader, C. Chemically programmed bispecific antibodies in diabody format Journal of Biological Chemistry 2016 291:19661-19673 DOI:10.1074/jbc.M116.745588 PMID:27445334 PMCID:PMC5016699
- Ewing, H., Fernandez-Vega, V., Spicer, T. P., Chase, P., Brown, S., Scampavia, L., Roush, W. R., Riley, S., Rosen, H., Hodder, P., Lambeau, G., Gelb, M. H. Fluorometric high-throughput screening assay for secreted phospholipases A(2) using phospholipid vesicles Journal of Biomolecular Screening 2016 21:713-721 DOI:10.1177/1087057116646742 PMID:27146384
- Pedzisa, L., Li, X., Rader, C., Roush, W. R. Assessment of reagents for selenocysteine conjugation and the stability of selenocysteine adducts Organic & Biomolecular Chemistry 2016 14:5141-5147 DOI:10.1039/c6ob00775a PMID:27184239 PMCID:PMC4887430
- Nair, R. N., Mishra, J. K., Li, F., Tortosa, M., Yang, C., Doherty, J. R., Cameron, M., Cleveland, J. L., Roush, W. R., Bannister, T. D. Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors MedChemComm 2016 7:900-905 DOI:10.1039/c5md00579e PMID:27347360
- Jones, B. D., Tochowicz, A., Tang, Y., Cameron, M. D., McCall, L. I., Hirata, K., Siqueira-Neto, J. L., Reed, S. L., McKerrow, J. H., Roush, W. R. Synthesis and evaluation of oxyguanidine analogues of the cysteine protease inhibitor WRR-483 against cruzain ACS Medicinal Chemistry Letters 2016 7:77-82 DOI:10.1021/acsmedchemlett.5600336 PMID:26819670 PMCID:PMC4716606
- Rosenberg, L. H., Lafitte, M., Quereda, V., Grant, W., Chen, W., Bibian, M., Noguchi, Y., Fallahi, M., Yang, C., Chang, J. C., Roush, W. R., Cleveland, J. L., et al. Therapeutic targeting of casein kinase 1δ in breast cancer Science Translational Medicine 2015 7:318ra202 DOI:10.1126/scitranslmed.aac8773 PMID:26676609 PMCID:PMC4809734
- Sanders, M. A., Madoux, F., Mladenovic, L., Zhang, H., Ye, X., Angrish, M., Mottillo, E. P., Caruso, J. A., Halvorsen, G., Roush, W. R., Chase, P., Hodder, P., et al. Endogenous and synthetic ABHD5 ligands regulate ABHD5-perilipin interactions and lipolysis in fat and muscle Cell Metabolism 2015 22:851-860 DOI:10.1016/j.cmet.2015.08.023 PMID:26411340 PMCID:PMC4862007
- Li, X., Patterson, J. T., Sarkar, M., Pedzisa, L., Kodadek, T., Roush, W. R., Rader, C. Site-specific dual antibody conjugation via engineered cysteine and selenocysteine residues Bioconjugate Chemistry 2015 26:2243-2248 DOI:10.1021/acs.bioconjchem.5600244 PMID:26161903
- Schreiber, S. L., Kotz, J. D., Li, M., Aube, J., Austin, C. P., Reed, J. C., Rosen, H., White, E. L., Sklar, L. A., Lindsley, C. W., Alexander, B. R., Bittker, J. A., et al. Advancing biological understanding and therapeutics discovery with small-molecule probes Cell 2015 161:1252-1265 DOI:10.1016/j.cell.2015.05.023 PMID:26046436 PMCID:PMC4564295
- El Hilali, X., Roush, W. R. Enantio- and diastereoselective synthesis of syn-β-hydroxy-α-alkenyl carboxamides via reductive aldol reactions of morpholine 4-methyl-2,3-pentadienoic carboxamide with diisopinocampheylborane Tetrahedron Letters 2015 56:3281-3284 DOI:10.1016/j.tetlet.2015.01.018
- Penas, C., Govek, E. E., Fang, Y., Ramachandran, V., Daniel, M., Wang, W., Maloof, M. E., Rahaim, R. J., Bibian, M., Kawauchi, D., Finkelstein, D., Han, J. L., et al. Casein kinase 1δ is an APC/C(Cdh1) substrate that regulates cerebellar granule cell neurogenesis Cell Reports 2015 11:249-260 DOI:10.1016/j.celrep.2015.03.016 PMID:25843713 PMCID:PMC4401652
- Ghalei, H., Schaub, F. X., Doherty, J. R., Noguchi, Y., Roush, W. R., Cleveland, J. L., Stroupe, M. E., Karbstein, K. Hrr25/CK1 delta-directed release of Ltv1 from pre-40S ribosomes is necessary for ribosome assembly and cell growth Journal of Cell Biology 2015 208:745-759 DOI:10.1083/jcb.201409056 PMID:25778921 PMCID:PMC4362465
- Wang, Y., Stowe, R. L., Pinello, C. E., Tian, G., Madoux, F., Li, D., Zhao, L. Y., Li, J. L., Wang, Y., Wang, Y., Ma, H., Hodder, P., et al. Identification of histone deacetylase inhibitors with benzoylhydrazide scaffold that selectively inhibit class I histone deacetylases Chemistry & Biology 2015 22:273-284 DOI:10.1016/j.chembiol.2014.12.015 PMID:25699604 PMCID:PMC4365786
- Corzo, C. A., Mari, Y., Chang, M. R., Khan, T., Kuruvilla, D., Nuhant, P., Kumar, N., West, G. M., Duckett, D. R., Roush, W. R., Griffin, P. R. Antiproliferation activity of a small molecule repressor of liver receptor homolog 1 Molecular Pharmacology 2015 87:296-304 DOI:10.1124/mol.114.095554 PMID:25473120 PMCID:PMC4293447
- Penas, C., Mishra, J. K., Wood, S. D., Schurer, S. C., Roush, W. R., Ayad, N. G. GSK3 inhibitors stabilize Wee1 and reduce cerebellar granule cell progenitor proliferation Cell Cycle 2015 14:417-424 DOI:10.4161/15384101.2014.974439 PMID:25616418 PMCID:PMC4353296
- Abbott, J. R., Allais, C., Roush, W. R. Preparattion of crystalline (diisopinocampheyl)borane Organic Syntheses 2015 92:26-37 DOI:10.15227/orgsyn.092.0026
- Abbott, J. R., Allais, C., Roush, W. R. Enantioselective reductive syn-aldol reactions of 4-acryloylmorpholine: preparation of (2R, 3S)-3-hydroxy-2-methyl-1-morpholino-5-phenylpentan-1-one Organic Syntheses 2015 92:38-57 DOI:10.15227/orgsyn.092.0038
- McCall, L. I., El Aroussi, A., Choi, J. Y., Vieira, D. F., De Muylder, G., Johnston, J. B., Chen, S., Kellar, D., Siqueira-Neto, J. L., Roush, W. R., Podust, L. M., McKerrow, J. H. Targeting Ergosterol biosynthesis in Leishmania donovani: essentiality of sterol 14 alpha-demethylase PLoS Neglected Tropical Diseases 2015 9 DOI:10.1371/journal.pntd.0003588 PMID:25768284 PMCID:PMC4359151
- Vieira, D. F., Choi, J. Y., Calvet, C. M., Siqueira-Neto, J. L., Johnston, J. B., Kellar, D., Gut, J., Cameron, M. D., McKerrow, J. H., Roush, W. R., Podust, L. M. Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51 Journal of Medicinal Chemistry 2014 57:10162-10175 DOI:10.1021/jm501568b PMID:25393646 PMCID:PMC4266343
- Choi, J. Y., Podust, L. M., Roush, W. R. Drug strategies targeting CYP51 in neglected tropical diseases Chemical Reviews 2014 114:11242-11271 DOI:10.1021/cr5003134 PMID:25337991 PMCID:PMC4254036
- Wang, H., Yang, C., Doherty, J. R., Roush, W. R., Cleveland, J. L., Bannister, T. D. Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors Journal of Medicinal Chemistry 2014 57:7317-7324 DOI:10.1021/jm500640x PMID:25068893 PMCID:PMC4161152
- Calvet, C. M., Vieira, D. F., Choi, J. Y., Kellar, D., Cameron, M. D., Siqueira-Neto, J. L., Gut, J., Johnston, J. B., Lin, L., Khan, S., McKerrow, J. H., Roush, W. R., et al. 4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency Journal of Medicinal Chemistry 2014 57:6989-7005 DOI:10.1021/jm500448u PMID:25101801 PMCID:PMC4148169
- Penas, C., Ramachandran, V., Simanski, S., Lee, C., Madoux, F., Rahaim, R. J., Chauhan, R., Barnaby, O., Schurer, S., Hodder, P., Steen, J., Roush, W. R., et al. Casein kinase 1 delta-dependent Wee1 protein degradation Journal of Biological Chemistry 2014 289:18893-18903 DOI:10.1074/jbc.M114.547661 PMID:24817118 PMCID:PMC4081930
- Vieira, D. F., Choi, J. Y., Roush, W. R., Podust, L. M. Expanding the binding envelope of CYP51 inhibitors targeting Trypanosoma cruzi with 4-aminopyridyl-based sulfonamide derivatives ChemBioChem 2014 15:1111-1120 DOI:10.1002/cbic.201402027 PMID:24771705 PMCID:PMC4091728
- Choi, J. Y., Calvet, C. M., Vieira, D. F., Gunatilleke, S. S., Cameron, M. D., McKerrow, J. H., Podust, L. M., Roush, W. R. R-configuration of 4-aminopyridyl-based inhibitors of CYP51 confers superior efficacy against Trypanosoma cruzi ACS Medicinal Chemistry Letters 2014 5:434-439 DOI:10.1021/ml500010m PMID:24900854 PMCID:PMC4027616
- Doherty, J. R., Yang, C., Scott, K. E. N., Cameron, M. D., Fallahi, M., Li, W., Hall, M. A., Amelio, A. L., Mishra, J. K., Li, F., Tortosa, M., Genau, H. M., et al. Blocking lactate export by inhibiting the Myc target MCT1 disables glycolysis and glutathione synthesis Cancer Research 2014 74:908-920 DOI:10.1158/0008-5472.can-13-2034 PMID:24285728 PMCID:PMC3946415
- Jiang, J., Taylor, A. B., Choi, J. Y., Hart, P. J., Roush, W. R., Fields, G. B., Hodder, P. S., Minong, D., Spicer, T. P. Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro Journal of Medicinal Chemistry 2014 57:9598-9611 DOI:10.1021/jm501284e PMID:25330343 PMCID:PMC4255739
- Allais, C., Tsai, A. S., Nuhant, P., Roush, W. R. Generation of stereochemically defined tetrasubstituted enolborinates by 1,4-hydroboration of α,β-unsaturated morpholine carboxamides with (diisopinocampheyl)borane Angewandte Chemie-International Edition 2013 52:12888-12891 DOI:10.1002/anie.201307302 PMID:24281884 PMCID:PMC3910328
- Kister, J., Ess, D. H., Roush, W. R. Enantio- and diastereoselective synthesis of syn-β-hydroxy-α-vinyl carboxylic esters via reductive aldol reactions of ethyl allenecarboxylate with 10-TMS-9-Borabicyclo[3.3.2]decane and DFT analysis of the hydroboration pathway Organic Letters 2013 15:5436-5439 DOI:10.1021/ol4025277 PMID:24138187 PMCID:PMC3849616
- Choi, J. Y., Calvet, C. M., Gunatilleke, S. S., Ruiz, C., Cameron, M. D., McKerrow, J. H., Podust, L. M., Roush, W. R. Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents Journal of Medicinal Chemistry 2013 56:7651-7668 DOI:10.1021/jm401067s PMID:24079662 PMCID:PMC3864028
- Nuhant, P., Allais, C., Roush, W. R. Diisopinocampheylborane-mediated reductive aldol reactions: highly enantio- and diastereoselective synthesis of syn aldols from N-acryloylmorpholine Angewandte Chemie-International Edition 2013 52:8703-8707 DOI:10.1002/anie.201302535 PMID:23818095 PMCID:PMC3813003
- Allais, C., Nuhant, P., Roush, W. R. (Diisopinocampheyl)borane-mediated reductive aldol reactions of acrylate esters: enantioselective synthesis of anti-aldols Organic Letters 2013 15:3922-3925 DOI:10.1021/ol401679g PMID:23885946 PMCID:PMC3773495
- Bibian, M., Rahaim, R. J., Choi, J. Y., Noguchi, Y., Schurer, S., Chen, W. M., Nakanishi, S., Licht, K., Rosenberg, L. H., Li, L., Feng, Y., Cameron, M. D., et al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties Bioorganic & Medicinal Chemistry Letters 2013 23:4374-4380 DOI:10.1016/j.bmcl.2013.05.075 PMID:23787102 PMCID:PMC3783656
- Chen, M., Roush, W. R. Enantioselective synthesis of (Z)- and (E)-2-methyl-1,5-anti-pentenediols via an allene hydroboration-double-allylboration reaction sequence Journal of the American Chemical Society 2013 135:9512-9517 DOI:10.1021/ja4033633 PMID:23758559 PMCID:PMC3733567
- Nuhant, P., Roush, W. R. Enantio- and diastereoselective synthesis of N-acetyl dihydrotetrafibricin methyl ester Journal of the American Chemical Society 2013 135:5340-5343 DOI:10.1021/ja401918r PMID:23530855 PMCID:PMC3679187
- Chen, M., Roush, W. R. Enantioselective synthesis of (E)-δ-silyl-anti-homoallylic alcohols via an enantiodivergent hydroboration-crotylboration reaction of a racemic allenylsilane Organic Letters 2013 15:1662-1665 DOI:10.1021/ol4004405 PMID:23534391 PMCID:PMC3663895
- Chen, M., Roush, W. R. Crotylboron-based synthesis of the polypropionate units of chaxamycins a/d, salinisporamycin, and rifamycin s Journal of Organic Chemistry 2013 78:3-8 DOI:10.1021/jo3008226 PMID:22703288 PMCID:PMC3465507
- Geist, J. G., Barth, R., Roush, W. R. Enantioselective synthesis of the C1-C11 fragment of tedanolide C Organic Letters 2013 15:58-61 DOI:10.1021/ol303089w PMID:23249423 PMCID:PMC3539184
- Abbott, J. R., Roush, W. R. Stereoselective synthesis of the disaccharide unit of incednine Organic Letters 2013 15:62-64 DOI:10.1021/ol303093z PMID:23249392 PMCID:PMC3537911
- Tsai, A. S., Chen, M., Roush, W. R. Chiral Brønsted acid catalyzed enantioselective synthesis of anti-homopropargyl alcohols via kinetic resolution-aldehyde allenylboration using racemic allenylboronates Organic Letters 2013 15:1568-1571 DOI:10.1021/ol4003459 PMID:23484801 PMCID:PMC3640598
- Chen, M., Roush, W. R. Enantiodivergent hydroboration reactions of a racemic allenylsilane with diisopinocampheylborane and Curtin-Hammett controlled double asymmetric crotylboration reactions of (S)-E-α-phenyldimethylsilyl(ddiisopinocampheyl)-crotylborane Tetrahedron 2013 69:5468-5475 DOI:10.1016/j.tet.2013.04.098 PMID:24039304 PMCID:PMC3768161
- Yang, H., Pinello, C. E., Luo, J., Li, D., Wang, Y., Zhao, L. Y., Jahn, S. C., Saldanha, S. A., Planck, J., Geary, K. R., Ma, H., Law, B. K., et al. Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents Molecular Cancer Therapeutics 2013 12:610-620 DOI:10.1158/1535-7163.mct-12-0930 PMID:23625935 PMCID:PMC3651759
- Dossey, A. T., Whitaker, J. M., Dancel, M. C. A., Vander Meer, R. K., Bernier, U. R., Gottardo, M., Roush, W. R. Defensive spiroketals from Asceles glaber (Phasmatodea): absolute configuration and effects on ants and mosquitoes Journal of Chemical Ecology 2012 38:1105-1115 DOI:10.1007/s10886-012-0183-x PMID:22976590 PMCID:PMC3473114
- Han, J. L., Chen, M., Roush, W. R. Diastereo- and enantioselective synthesis of (E)-2-Methyl-1,2-syn- and (E)-2-Methyl-1,2-anti-3-pentenediols via allenylboronate kinetic resolution with ((d)Ipc)2BH and aldehyde allylboration Organic Letters 2012 14:3028-3031 DOI:10.1021/ol3010968 PMID:22646839 PMCID:PMC3426628
- Chen, M., Roush, W. R. Enantioselective synthesis of (+)-crocacin C. An example of a highly challenging mismatched double asymmetric δ-stannylcrotylboration reaction Organic Letters 2012 14:1880-1883 DOI:10.1021/ol300476f PMID:22409510 PMCID:PMC3321065
- Chen, M., Roush, W. R. Enantioselective synthesis of (-)-basiliskamide A Organic Letters 2012 14:1556-1559 DOI:10.1021/ol300282e PMID:22372693 PMCID:PMC3306514
- Chen, M., Roush, W. R. Highly stereoselective synthesis of anti,anti-dipropionate stereotriads: a solution to the long-standing problem of challenging mismatched double asymmetric crotylboration reactions Journal of the American Chemical Society 2012 134:3925-3931 DOI:10.1021/ja300472a PMID:22332989 PMCID:PMC3292054
- Choi, J. Y., Plummer, M. S., Starr, J., Desbonnet, C. R., Soutter, H., Chang, J., Miller, J. R., Dillman, K., Miller, A. A., Roush, W. R. Structure guided development of novel thymidine mimetics targeting Pseudomonas aeruginosa thymidylate kinase: from hit to lead generation Journal of Medicinal Chemistry 2012 55:852-870 DOI:10.1021/jm201349f PMID:22243413 PMCID:PMC3306445
- Chen, M., Roush, W. R. Total synthesis of (-)-tirandamycin C Organic Letters 2012 14:426-428 DOI:10.1021/ol203161u PMID:22148850 PMCID:PMC3253220
- Chen, M., Roush, W. R. Enantioselective synthesis of anti- and syn-homopropargyl alcohols via chiral Brønsted acid catalyzed asymmetric allenylboration reactions Journal of the American Chemical Society 2012 134:10947-10952 DOI:10.1021/ja3031467 PMID:22731887 PMCID:PMC3474359
- Ying, M. B., Roush, W. R. Studies on the synthesis of reidispongiolide A: stereoselective synthesis of the C(22)-C(36) fragment Tetrahedron 2011 67:10274-10280 DOI:10.1016/j.tet2011.10.029 PMID:22711935 PMCID:PMC3375686
- Roth, J., Minond, D., Darout, E., Liu, Q., Lauer, J., Hodder, P., Fields, G. B., Roush, W. R. Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds Bioorganic & Medicinal Chemistry Letters 2011 21:7180-7184 DOI:10.1016/j.bmcl.2011.09.077 PMID:22018790 PMCID:PMC3210410
- Zhou, Y. C., Agudelo, J., Lu, K., Goetz, D. H., Hansell, E., Chen, Y. T., Roush, W. R., McKerrow, J., Craik, C. S., Amberg, S. M., Simmons, G. Inhibitors of SARS-CoV entry: identification using an internally-controlled dual envelope pseudovirion assay Antiviral Research 2011 92:187-194 DOI:10.1016/j.antiviral.2011.07.016 PMID:21820471 PMCID:PMC3205982
- Nuhant, P., Kister, J., Lira, R., Sorg, A., Roush, W. R. Development of a double allylboration reagent targeting 1,5-syn-(E)-diols: application to the synthesis of the C(23)-C(40) fragment of tetrafibricin Tetrahedron 2011 67:6497-6512 DOI:10.1016/j.tet.2011.06.008 PMID:21857752 PMCID:PMC3156408
- Busby, S. A., Kumar, N., Kuruvilla, D. S., Istrate, M. A., Conkright, J. J., Wang, Y. J., Kamenecka, T. M., Cameron, M. D., Roush, W. R., Burris, T. P., Griffin, P. R. Identification of a novel non-retinoid pan inverse agonist of the retinoic acid receptors ACS Chemical Biology 2011 6:618-627 DOI:10.1021/cb100396s PMID:21381756 PMCID:PMC3117942
- Sun, H. K., Abbott, J. R., Roush, W. R. Stereoselective synthesis of a model C(18)-C(35) spiroketal fragment of integramycin Organic Letters 2011 13:2734-2737 DOI:10.1021/ol200834p PMID:21510632 PMCID:PMC3094501
- Lee, Y., Choi, J. Y., Fu, H., Harvey, C., Ravindran, S., Roush, W. R., Boothroyd, J. C., Khosla, C. Chemistry and biology of macrolide antiparasitic agents Journal of Medicinal Chemistry 2011 54:2792-2804 DOI:10.1021/jm101593u PMID:21428405 PMCID:PMC3085955
- Solt, L. A., Kumar, N., Nuhant, P., Wang, Y. J., Lauer, J. L., Liu, J., Istrate, M. A., Kamenecka, T. M., Roush, W. R., Vidovic, D., Schurer, S. C., Xu, J. H., et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand Nature 2011 472:491-494 DOI:10.1038/nature10075 PMID:21499262 PMCID:PMC3148894
- Halvorsen, G. T., Roush, W. R. Stereoselective synthesis of the decahydrofluorene core of the hirsutellones Tetrahedron Letters 2011 52:2072-2075 DOI:10.1016/j.tetlet.2010.10.111 PMID:21503271 PMCID:PMC3077760
- Chen, M., Roush, W. R. Enantioconvergent hydroboration of a racemic allene: enantioselective synthesis of (E)-δ-stannyl-anti-homoallylic alcohols via aldehyde crotylboration Journal of the American Chemical Society 2011 133:5744-5747 DOI:10.1021/ja2010187 PMID:21449594 PMCID:PMC3086366
- Chen, M., Roush, W. R. Enantioselective syntheses of syn- and anti-beta-hydroxyallyisilanes via allene hydroboration-aldehyde allylboration reactions Organic Letters 2011 13:1992-1995 DOI:10.1021/ol200392u PMID:21410173 PMCID:PMC3075570
- Kister, J., Nuhant, P., Lira, R., Sorg, A., Roush, W. R. Enantio- and diastereoselective synthesis of (E)-1,5-syn-diols: application to the synthesis of the C(23)-C(40) fragment of tetrafibricin Organic Letters 2011 13:1868-1871 DOI:10.1021/ol2003836 PMID:21375316 PMCID:PMC3064748
- Stewart, P. S., Chen, M., Roush, W. R., Ess, D. H. Thermodynamic control of 1,3-boratropic shifts of α- and γ-stannyl-substituted allylboranes: hyperconjugation outweighs steric effects Organic Letters 2011 13:1478-1481 DOI:10.1021/ol2001599 PMID:21323387 PMCID:PMC3462665
- Kumar, N., Kojetin, D. J., Solt, L. A., Kumar, K. G., Nuhant, P., Duckett, D. R., Cameron, M. D., Butler, A. A., Roush, W. R., Griffin, P. R., Burris, T. P. Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist ACS Chemical Biology 2011 6:218-222 DOI:10.1021/cb1002762 PMID:21090593 PMCID:PMC3076127
- Sun, H., Roush, W. R. Synthesis of (+)-B-allyldiisopinocampheylborane and its reaction with aldehydes Organic Syntheses 2011 88:87-101 DOI:10.1002/0471264229.os088.09 PMID:22962503
- Sun, H., Roush, W. R. Synthesis of (S,S)-diisopropyl tartrate (E)-crotylboronate and its reaction with aldehydes: (2R,3R,4R)-1,2-dideoxy-2-ethenyl-4,5-O-(1-methylethylidene)xylitol Organic Syntheses 2011 88:181-196 DOI:10.1002/0471264229.os088.17 PMID:21666877
- Wang, Y. J., Kumar, N., Nuhant, P., Cameron, M. D., Istrate, M. A., Roush, W. R., Griffin, P. R., Burris, T. P. Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ ACS Chemical Biology 2010 5:1029-1034 DOI:10.1021/cb100223d PMID:20735016 PMCID:PMC3003750
- Gianni, D., Taulet, N., Zhang, H., DerMardirossian, C., Kister, J., Martinez, L., Roush, W. R., Brown, S. J., Bokoch, G. M., Rosen, H. A novel and specific NADPH oxidase-1 (Nox1) small-molecule inhibitor blocks the formation of functional invadopodia in human colon cancer cells ACS Chemical Biology 2010 5:981-993 DOI:10.1021/cb100219n PMID:20715845 PMCID:PMC2955773
- Winbush, S. M., Roush, W. R. Enantioselective synthesis of (Z)-1,2-anti-2,5-anti-triol monosilyl ethers using a cross-metathesis allylboration sequence Organic Letters 2010 12:4344-4347 DOI:10.1021/ol101789g PMID:20806914 PMCID:PMC2945398
- Madoux, F., Simanski, S., Chase, P., Mishra, J. K., Roush, W. R., Ayad, N. G., Hodder, P. An ultra-high throughput cell-based screen for wee1 degradation inhibitors Journal of Biomolecular Screening 2010 15:907-917 DOI:10.1177/1087057110375848 PMID:20660794 PMCID:PMC3082437
- Chen, Y. T., Brinen, L. S., Kerr, I. D., Hansell, E., Doyle, P. S., McKerrow, J. H., Roush, W. R. In vitro and in vivo studies of the trypanocidal properties of WRR-483 against Trypanosoma cruzi PLoS Neglected Tropical Diseases 2010 4:e825 DOI:10.1371/journal.pntd.0000825 PMID:20856868 PMCID:PMC2939063
- Chen, M., Roush, W. R. Highly (E)-selective BF(3).Et(2)O-promoted allylboration of chiral nonracemic alpha-substituted allylboronates and analysis of the origin of stereocontrol Organic Letters 2010 12:2706-2709 DOI:10.1021/ol1007444 PMID:20476769 PMCID:PMC2891445
- Chen, M., Ess, D. H., Roush, W. R. Enantioselective synthesis of (E)-delta-stannyl homoallylic alcohols via aldehyde allylboration using alpha-stannylallylboranes generated by allene hydroboration followed by a highly diastereoselective 1,3-boratropic shift Journal of the American Chemical Society 2010 132:7881-7883 DOI:10.1021/ja103041u PMID:20496899 PMCID:PMC2890212
- He, C., Nora, G. P., Schneider, E. L., Kerr, I. D., Hansell, E., Hirata, K., Gonzalez, D., Sajid, M., Boyd, S. E., Hruz, P., Cobo, E. R., Le, C., et al. A novel Entamoeba histolytica cysteine proteinase, EhCP4, is key for invasive amebiasis and a therapeutic target Journal of Biological Chemistry 2010 285:18516-18527 DOI:10.1074/jbc.M109.086181 PMID:20378535 PMCID:PMC2881777
- Barth, R., Roush, W. R. Enantioselective synthesis of alpha-methylene-beta-hydroxy carboxylic acid derivatives via a diastereoselective aldol/beta-elimination sequence: application to the C(15)-C(21) fragment of tedanolide C Organic Letters 2010 12:2342-2345 DOI:10.1021/ol1006955 PMID:20405855 PMCID:PMC2872132
- Ess, D. H., Kister, J., Chen, M., Roush, W. R. Origin of thermodynamic versus kinetic control of allene hydroboration with 9-borabicyclo[3.3.1]nonane and 10(R)-trimethylsilyl-9-borabicyclo[3.3.2]decane Organic Letters 2009 11:5538-5541 DOI:10.1021/ol902364d PMID:19899749 PMCID:PMC2803353
- Ess, D. H., Kister, J., Chen, M., Roush, W. R. Quantum-mechanical study of 10-R-9-borabicyclo[3.3.2]decane alkene hydroboration Journal of Organic Chemistry 2009 74:8626-8637 DOI:10.1021/jo901737d PMID:19824624 PMCID:PMC2803351
- Chen, M., Handa, M., Roush, W. R. Enantioselective synthesis of 2-methyl-1,2-syn- and 2-methyl-1,2-anti-3-butenediols via allene hydroboration-aldehyde allylboration reaction sequences Journal of the American Chemical Society 2009 131:14602-14603 DOI:10.1021/ja904599h PMID:19778012 PMCID:PMC2762002
- Kister, J., DeBaillie, A. C., Lira, R., Roush, W. R. Stereoselective synthesis of gamma-substituted (Z)-allylic boranes via kinetically controlled hydroboration of allenes with 10-TMS-9-borabicyclo[3.3.2]decane Journal of the American Chemical Society 2009 131:14174-14175 DOI:10.1021/ja905494c PMID:19775159 PMCID:PMC2767336
- Dossey, A. T., Gottardo, M., Whitaker, J. M., Roush, W. R., Edison, A. S. Alkyldimethylpyrazines in the defensive spray of Phyllium westwoodii: a first for order Phasmatodea Journal of Chemical Ecology 2009 35:861-870 DOI:10.1007/s10886-009-9666-9 PMID:19685263 PMCID:PMC3787517
- Li, F. Z., Roush, W. R. Stereloselective synthesis of syn,syn- and syn,anti-1,3,5-triols via intramolecular hydrosilylation of substituted pent-3-en-1,5-diols Organic Letters 2009 11:2932-2935 DOI:10.1021/ol9009877 PMID:19507846 PMCID:PMC2755244
- Tortosa, M., Yakelis, N. A., Roush, W. R. Total synthesis of (+)-superstolide A Journal of Organic Chemistry 2008 73:9657-9667 DOI:10.1021/jo801794s PMID:18956845 PMCID:PMC2736345
- Dunetz, J. R., Julian, L. D., Newcom, J. S., Roush, W. R. Total syntheses of (+)-tedanolide and (+)-13-deoxytedanolide Journal of the American Chemical Society 2008 130:16407-16416 DOI:10.1021/ja8063205 PMID:18980317 PMCID:PMC2645944
- Halvorsen, G. T., Roush, W. R. Siloxacyclopentenes as dienophile-linked directing groups in intramolecular Diels-Alder reactions Organic Letters 2008 10:5313-5316 DOI:10.1021/ol802266s PMID:18954061 PMCID:PMC2650085
- Chen, Y. T., Lira, R., Hansell, E., McKerrow, J. H., Roush, W. R. Synthesis of macrocyclic trypanosomal cysteine protease inhibitors Bioorganic & Medicinal Chemistry Letters 2008 18:5860-5863 DOI:10.1016/j.bmcl.2008.06.012 PMID:18585034 PMCID:PMC2642929
- Bates, R. H., Chen, M., Roush, W. R. Applications of chiral allylmetallating agents toward the synthesis of oxygen heterocycles Current Opinion in Drug Discovery & Development 2008 11:778-792 PMID:18946843
- Pragani, R., Roush, W. R. Studies on the synthesis of durhamycin A: stereoselective synthesis of a model aglycone Organic Letters 2008 10:4613-4616 DOI:10.1021/ol8018727 PMID:18808128 PMCID:PMC2626543
- Bates, R. H., Shotwell, J. B., Roush, W. R. Stereoselective syntheses of the C(1)-C(9) fragment of amphidinolide C Organic Letters 2008 10:4343-4346 DOI:10.1021/ol801852j PMID:18783230 PMCID:PMC2650083
- Huh, C. W., Roush, W. R. Highly stereoselective and modular syntheses of 10-hydroxytrilobacin and three diastereomers via stereodivergent [3 + 2]-annulation reactions Organic Letters 2008 10:3371-3374 DOI:10.1021/ol801242d PMID:18588305
- Roush, W. R. Total synthesis of biologically active natural products Journal of the American Chemical Society 2008 130:6654-6656 DOI:10.1021/ja8028813 PMID:18491856
- Dunetz, J. R., Roush, W. R. Concerning the synthesis of the tedanolide C(13)-C(23) fragment via anti-aldol reaction Organic Letters 2008 10:2059-2062 DOI:10.1021/ol800546g PMID:18422319
- Roth, J., Madoux, F., Hodder, P., Roush, W. R. Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds Bioorganic & Medicinal Chemistry Letters 2008 18:2628-2632 DOI:10.1016/j.bmcl.2008.03.027 PMID:18374567 PMCID:PMC2592603
- Winbush, S. M., Mergott, D. J., Roush, W. R. Total synthesis of (-)-spinosyn A: examination of structural features that govern the stereoselectivity of the key transannular Diels-Alder reaction Journal of Organic Chemistry 2008 73:1818-1829 DOI:10.1021/jo7024515 PMID:18215065
- Tortosa, M., Yakelis, N. A., Roush, W. R. Total synthesis of (+)-superstolide A Journal of the American Chemical Society 2008 130:2722-2723 DOI:10.1021/ja710238h PMID:18254629
- Hicks, J. D., Roush, W. R. Synthesis of the C(26)-C(42) and C(43)-C(67) pyran-containing fragments of amphidinol 3 via a common pyran intermediate Organic Letters 2008 10:681-684 DOI:10.1021/ol703042q PMID:18205377
- Handa, M., Scheidt, K. A., Bossart, M., Zheng, N., Roush, W. R. Studies on the synthesis of apoptolidin A. 1. Synthesis of the C(1)-C(11) fragment Journal of Organic Chemistry 2008 73:1031-1035 DOI:10.1021/jo702250z PMID:18163645
- Handa, M., Smith, W. J., Roush, W. R. Studies on the synthesis of apoptolidin A. 2. Synthesis of the disaccharide unit Journal of Organic Chemistry 2008 73:1036-1039 DOI:10.1021/jo7022526 PMID:18163646
- Hicks, J. D., Huh, C. W., Legg, A. D., Roush, W. R. Concerning the selective protection of (Z)-1,5-syn-ene-diols and (E)-1,5-anti-ene-diols as allylic triethylsilyl ethers Organic Letters 2007 9:5621-5624 DOI:10.1021/ol702588h PMID:18027963 PMCID:PMC2504016
- Lira, R., Roush, W. R. Enantio- and diastereoselective synthesis of syn-beta-hydroxyallylsilanes via a chiral (Z)-gamma-silylallylboronate Organic Letters 2007 9:4315-4318 DOI:10.1021/ol7018746 PMID:17867698
- Goetz, D. H., Choe, Y., Hansell, E., Chen, Y. T., McDowell, M., Jonsson, C. B., Roush, W. R., McKerrow, J., Craik, C. S. Substrate specificity profiling and identification of a new class of inhibitor for the major protease of the SARS coronavirus Biochemistry 2007 46:8744-8752 DOI:10.1021/bi0621415 PMID:17605471
- Melendez-Lopez, S. G., Herdman, S., Hirata, K., Choi, M. H., Choe, Y., Craik, C., Caffrey, C. R., Hansell, E., Chavez-Munguia, B., Chen, Y. T., Roush, W. R., McKerrow, J., et al. Use of recombinant Entamoeba histolytica cysteine proteinase 1 to identify a potent inhibitor of amebic invasion in a human colonic model Eukaryotic Cell 2007 6:1130-1136 DOI:10.1128/ec.00094-07 PMID:17513563 PMCID:PMC1951106
- Va, P., Roush, W. R. Total synthesis of amphidinolide E and amphidinolide E stereoisomers Tetrahedron 2007 63:5768-5796 DOI:10.1016/j.tet.2007.02.058 PMID:18575572 PMCID:PMC2031846
- Halvorsen, G. T., Roush, W. R. Intramolecular Diels-Alder reactions of siloxacyclopentene constrained trienes Organic Letters 2007 9:2243-2246 DOI:10.1021/ol070858u PMID:17480094 PMCID:PMC2504012
- Lira, R., Roush, W. R. Stereoselective synthesis of the C(1)-C(19) fragment of tetrafibricin Organic Letters 2007 9:533-536 DOI:10.1021/ol0629869 PMID:17249805 PMCID:PMC2701644
- Va, P., Roush, W. R. Synthesis of 2-epi-amphidinolide E: an unexpected and highly selective C(2)inversion during an esterification reaction Organic Letters 2007 9:307-310 DOI:10.1021/ol0628098 PMID:17217291 PMCID:PMC2593877
- Va, P., Roush, W. R. Total synthesis of amphidinolide E Journal of the American Chemical Society 2006 128:15960-15961 DOI:10.1021/ja066663j PMID:17165709 PMCID:PMC2538580
- Trullinger, T. K., Qi, J., Roush, W. R. Studies on the synthesis of quartromicins A(3) and D(3): synthesis of the vertical and horizontal bis-spirotetronate fragments Journal of Organic Chemistry 2006 71:6915-6922 DOI:10.1021/jo061059c PMID:16930045 PMCID:PMC2593838
- Qi, J., Roush, W. R. Synthesis of precursors of the agalacto (exo) fragment of the quartromicins via an auxiliary-controlled exo-selective Diels-Alder reaction Organic Letters 2006 8:2795-2798 DOI:10.1021/ol0609208 PMID:16774259 PMCID:PMC2515626
- Thalji, R. K., Roush, W. R. Remarkable phosphine-effect on the intramolecular aldol reactions of unsaturated 1,5-diketones: highly regioselective synthesis of cross-conjugated dienones Journal of the American Chemical Society 2005 127:16778-16779 DOI:10.1021/ja0540851 PMID:16316211 PMCID:PMC2515627
- Lambert, W. T., Roush, W. R. Synthesis of the A-B subunit of angelmicin B Organic Letters 2005 7:5501-5504 DOI:10.1021/ol052321r PMID:16288541
- Hicks, J. D., Flamme, E. M., Roush, W. R. Synthesis of the C(43)-C(67) fragment of amphidinol 3 Organic Letters 2005 7:5509-5512 DOI:10.1021/ol052322j PMID:16288543
- Mertz, E., Tinsley, J. M., Roush, W. R. [3 + 2]-annulation reactions of chiral allylsilanes and chiral aldehydes. Studies on the synthesis of bis-tetrahydrofuran substructures of annonaceous acetogenins Journal of Organic Chemistry 2005 70:8035-8046 DOI:10.1021/jo0511290 PMID:16277325
- Tinsley, J. M., Mertz, E., Chong, P. Y., Rarig, R. A. F., Roush, W. R. Synthesis of (+)-bullatacin via the highly diastereoselective [3+2] annulation reaction of a racemic aldehyde and a nonracemic allylsilane Organic Letters 2005 7:4245-4248 DOI:10.1021/ol051719k PMID:16146398 PMCID:PMC2507730
- Owen, R. M., Roush, W. R. Stereoselective synthesis of the C(1)-C(11) fragment of peloruside A Organic Letters 2005 7:3941-3944 DOI:10.1021/ol0514303 PMID:16119937
- Flamme, E. M., Roush, W. R. Synthesis of 2,6-trans-disubstituted 5,6-dihydropyrans from (Z)-1,5-syn-endiols Beilstein Journal of Organic Chemistry 2005 1:7 DOI:10.1186/1860-5397-1-7 PMID:16542020 PMCID:PMC1399455
- Tinsley, J. M., Roush, W. R. Total synthesis of asimicin via highly stereoselective [3 + 2] annulation reactions of substituted allylsilanes Journal of the American Chemical Society 2005 127:10818-10819 DOI:10.1021/ja051986l PMID:16076173
- Heitzman, C. L., Lambert, W. T., Mertz, E., Shotwell, J. B., Tinsley, J. M., Va, P., Roush, W. R. Efficient protiodesilylation of unactivated C(sp3)-SiMe2Ph bonds using tetrabutylammonium fluoride Organic Letters 2005 7:2405-2408 DOI:10.1021/ol0506821 PMID:15932209 PMCID:PMC2515625
- Julian, L. D., Newcom, J. S., Roush, W. R. Total synthesis of (+)-13-deoxytedanolide Journal of the American Chemical Society 2005 127:6186-6187 DOI:10.1021/ja050729d PMID:15853320
- Liu, C. M., Smith, W. J., Gustin, D. J., Roush, W. R. Experimental evidence for chair-like transition states in aldol reactions of methyl ketone lithium enolates: stereoselective synthesis and utilization of a deuterium-labeled enolate as a probe of reaction stereochemistry Journal of the American Chemical Society 2005 127:5770-5771 DOI:10.1021/ja050730c PMID:15839658
- Dineen, T. A., Roush, W. R. Stereoselective synthesis of the octahydronaphthalene unit of integramycin via an intramolecular Diels-Alder reaction Organic Letters 2005 7:1355-1358 DOI:10.1021/ol050191g PMID:15787505
- Flamme, E. M., Roush, W. R. Synthesis of the C(1)-C(25) fragment of amphidinol 3: application of the double-allylboration reaction for synthesis of 1,5-diols Organic Letters 2005 7:1411-1414 DOI:10.1021/ol050250q PMID:15787519
- Dias, L. C., Aguilar, A. M., Salles, A. G., Steil, L. J., Roush, W. R. Concerning the application of the 1H NMR ABX analysis for assignment of stereochemistry to aldols deriving from aldehydes lacking beta-branches Journal of Organic Chemistry 2005 70:10461-10465 DOI:10.1021/jo051773e PMID:16323858
- Narayan, S., Roush, W. R. Studies toward the total synthesis of angelmicin B (hibarimicin B): synthesis of a model CD-D' arylnaphthoquinone Organic Letters 2004 6:3789-3792 DOI:10.1021/ol048436x PMID:15469350
- Shotwell, J. B., Roush, W. R. Synthesis of the C11-C29 fragment of amphidinolide F Organic Letters 2004 6:3865-3868 DOI:10.1021/ol048381z PMID:15469369
- Mergott, D. J., Frank, S. A., Roush, W. R. Total synthesis of (-)-spinosyn A Proceedings of the National Academy of Sciences of the United States of America 2004 101:11955-11959 DOI:10.1073/pnas.0401247101 PMID:15173590 PMCID:PMC514415
- Durham, T. B., Blanchard, N., Savall, B. M., Powell, N. A., Roush, W. R. Total synthesis of formamicin Journal of the American Chemical Society 2004 126:9307-9317 DOI:10.1021/ja048493i PMID:15281821
- Methot, J. L., Roush, W. R. Nucleophilic phosphine organocatalysis Advanced Synthesis & Catalysis 2004 346:1035-1050 DOI:10.1002/adsc.200404087
- Roush, W. R., Neitz, R. J. Studies on the synthesis of landomycin A. Synthesis of the originally assigned structure of the aglycone, landomycinone, and revision of structure Journal of Organic Chemistry 2004 69:4906-4912 DOI:10.1021/jo049426c PMID:15255715
- Dineen, T. A., Roush, W. R. Total synthesis of cochleamycin A Organic Letters 2004 6:2043-2046 DOI:10.1021/ol049331x PMID:15176814
- Roush, W. R. Recent studies in carbonyl allylation reactions: application to the synthesis of oxygen heterocycles Actualite Chimique 2004 21-22
- Coppola, B. P., Roush, W. R. Broadening the existing intergenerational structure of scholarly development in chemistry Peer Review 2004 6:19
- Dineen, T. A., Roush, W. R. Probing the Lewis acid-catalyzed intramolecular Diels-Alder cyclizations of allylic alkoxy-substituted (Z)-1,3-dienes Organic Letters 2003 5:4725-4728 DOI:10.1021/ol035900+ PMID:14627425
- Methot, J. L., Roush, W. R. Synthetic studies toward FR182877. Remarkable solvent effect in the vinylogous morita-baylis-hillman cyclization Organic Letters 2003 5:4223-4226 DOI:10.1021/ol0357550 PMID:14572290
- Boitano, A., Emal, C. D., Leonetti, F., Blatt, N. B., Dineen, T. A., Ellman, J. A., Roush, W. R., Opipari, A. W., Glick, G. D. Structure activity studies of a novel cytotoxic benzodiazepine Bioorganic & Medicinal Chemistry Letters 2003 13:3327-3330 DOI:10.1016/s0960-894x(03)00683-8 PMID:12951119
- Reddick, J. J., Cheng, J. M., Roush, W. R. Relative rates of Michael reactions of 2'-(phenethyl)thiol with vinyl sulfones, vinyl sulfonate esters, and vinyl sulfonamides relevant to vinyl sulfonyl cysteine protease inhibitors Organic Letters 2003 5:1967-1970 DOI:10.1021/ol034555l PMID:12762698
- Durham, T. B., Roush, W. R. Stereoselective synthesis of 2-deoxy-beta-galactosides via 2-deoxy-2-bromo- and 2-deoxy-2-iodo-galactopyranosyl donors Organic Letters 2003 5:1871-1874 DOI:10.1021/ol034393t PMID:12762674
- Durham, T. B., Roush, W. R. Stereoselective synthesis of functionalized precursors of the CDEF and CDE 2,6-dideoxy-tetra- and trisaccharide units of durhamycins A and B Organic Letters 2003 5:1875-1878 DOI:10.1021/ol034395d PMID:12762675
- Yakelis, N. A., Roush, W. R. Synthesis of the C(21)-C(26) fragment of superstolide A: concerning the stereochemistry of (E)-crotylboration reactions of alaninal derivatives Journal of Organic Chemistry 2003 68:3838-3843 DOI:10.1021/jo0341012 PMID:12737561
- Heo, J. N., Holson, E. B., Roush, W. R. Common-intermediate strategy for synthesis of conduritols and inositols via beta-hydroxy cyclohexenylsilanes Organic Letters 2003 5:1697-1700 DOI:10.1021/ol034349d PMID:12735755
- Heo, J. N., Micalizio, G. C., Roush, W. R. Enantio- and diastereoselective synthesis of cyclic beta-hydroxy allylsilanes via sequential aldehyde gamma-silylallylboration and ring-closing metathesis reactions Organic Letters 2003 5:1693-1696 DOI:10.1021/ol034347t PMID:12735754
- Chemler, S. R., Roush, W. R. Stereochemistry of the allylation and crotylation reactions of alpha-methyl-beta-hydroxy aldehydes with allyl- and crotyltrifluorosilanes. Synthesis of anti, anti-dipropionate stereotriads and stereodivergent pathways for the reactions with 2,3-anti- and 2,3-syn-alpha-methyl-beta-hydroxy aldehydes Journal of Organic Chemistry 2003 68:1319-1333 DOI:10.1021/jo0267908 PMID:12585871
- Savall, B. M., Blanchard, N., Roush, W. R. Total synthesis of the formamicin aglycon, formamicinone Organic Letters 2003 5:377-379 DOI:10.1021/ol027569k PMID:12556196
- Blanchard, N., Roush, W. R. 2-deoxy-2-iodo-beta-glucopyranosyl fluorides: mild and highly stereoselective glycosyl donors for the synthesis of 2-deoxy-beta-glycosides from beta-hydroxy ketones Organic Letters 2003 5:81-84 DOI:10.1021/ol027257h PMID:12509896
- Shenai, B. R., Lee, B. J., Alvarez-Hernandez, A., Chong, P. Y., Emal, C. D., Neitz, R. J., Roush, W. R., Rosenthal, P. J. Structure-activity relationships for inhibition of cysteine protease activity and development of Plasmodium falciparum by peptidyl vinyl sulfones Antimicrobial Agents and Chemotherapy 2003 47:154-160 DOI:10.1128/aac.47.1.154-160.2003 PMID:12499184 PMCID:PMC149004
- Roush, W. R., Newcom, J. S. Studies on the synthesis of tedanolide. 2. Stereoselective synthesis of a protected C(1)-C(12) fragment Organic Letters 2002 4:4739-4742 DOI:10.1021/ol0272343 PMID:12489975
- Chong, P. Y., Roush, W. R. Concerning the origin of the high beta-selectivity of glycosidation reactions of 2-deoxy-2-iodo-glucopyranosyl trichloroacetimidates Organic Letters 2002 4:4523-4526 DOI:10.1021/ol027066e PMID:12465928
- Roush, W. R., Chen, H., Reilly, M. L. Studies on the synthesis of kijanolide: synthesis of an advanced seco-acid intermediate Heterocycles 2002 58:259-282 DOI:10.3987/COM-02-S(M)17
- Flamme, E. M., Roush, W. R. Enantioselective synthesis of 1,5-anti- and 1,5-syn-diols using a highly diastereoselective one-pot double allylboration reaction sequence Journal of the American Chemical Society 2002 124:13644-13645 DOI:10.1021/ja028055j PMID:12431072
- Holson, E. B., Roush, W. R. Diastereoselective synthesis of the C(17)-C(28) fragment (the C-D spiroketal unit) of spongistatin 1 (altohyrtin A) via a kinetically controlled iodo-spiroketalization reaction Organic Letters 2002 4:3719-3722 DOI:10.1021/ol0266875 PMID:12375927
- Holson, E. B., Roush, W. R. Synthesis of the C(2)-C(13) fragment (the A-B spiroketal unit) of spongistatin 1 (altohyrtin A): use of a common intermediate for the synthesis of both spongistatin spiroketals Organic Letters 2002 4:3723-3725 DOI:10.1021/ol026688x PMID:12375928
- Gung, B. W., Xue, X. W., Roush, W. R. The origin of diastereofacial control in allylboration reactions using tartrate ester derived allylboronates: attractive interactions between the Lewis acid coordinated aldehyde carbonyl group and an ester carbonyl oxygen Journal of the American Chemical Society 2002 124:10692-10697 DOI:10.1021/ja026373c PMID:12207523
- Mergott, D. J., Frank, S. A., Roush, W. R. Application of the intramolecular vinylogous Morita-Baylis-Hillman reaction toward the synthesis of the spinosyn A tricyclic nucleus Organic Letters 2002 4:3157-3160 DOI:10.1021/ol026540d PMID:12201741
- Roush, W. R., Barda, D. A., Limberakis, C., Kunz, R. K. Studies on the synthesis of the quartromicins: partial stereochemical assignment of quartromicins a(3) and d-3 and diastereoselective synthesis of the endo- and exo-spirotetronate subunits Tetrahedron 2002 58:6433-6454 DOI:10.1016/s0040-4020(02)00656-7
- Hernandez, A. A., Roush, W. R. Recent advances in the synthesis, design and selection of cysteine protease inhibitors Current Opinion in Chemical Biology 2002 6:459-465 DOI:10.1016/s1367-5931(02)00345-9 PMID:12133721
- Roush, W. R., Hertel, L., Schnaderbeck, M. J., Yakelis, N. A. Synthesis of the C(18)-(C26) segment of superstolide A Tetrahedron Letters 2002 43:4885-4887 DOI:10.1016/s0040-4039(02)00903-6
- Scheidt, K. A., Bannister, T. D., Tasaka, A., Wendt, M. D., Savall, B. M., Fegley, G. J., Roush, W. R. Total synthesis of (-)-bafilomycin A(1) Journal of the American Chemical Society 2002 124:6981-6990 DOI:10.1021/ja017885e PMID:12059221
- Roush, W. R., Bannister, T. D., Wendt, M. D., VanNieuwenhze, M. S., Gustin, D. J., Dilley, G. J., Lane, G. C., Scheidt, K. A., Smith, W. J. An NMR method for assigning relative stereochemistry to beta-hydroxy ketones deriving from aldol reactions of methyl ketones Journal of Organic Chemistry 2002 67:4284-4289 DOI:10.1021/jo0164148 PMID:12054964
- Frank, S. A., Roush, W. R. Studies on the synthesis of (-)-spinosyn A: application of the steric directing group strategy to transannular Diels-Alder reactions Journal of Organic Chemistry 2002 67:4316-4324 DOI:10.1021/jo025580s PMID:12054969
- Roush, W. R., Bannister, T. D., Wendt, M. D., Jablonowski, J. A., Scheidt, K. A. Studies on the synthesis of bafilomycin A(1): stereochemical aspects of the fragment assembly aldol reaction for construction of the C(13)-C25) segment Journal of Organic Chemistry 2002 67:4275-4283 DOI:10.1021/jo016413f PMID:12054963
- Frank, S. A., Mergott, D. J., Roush, W. R. The vinylogous intramolecular Morita-Baylis-Hillman reaction: synthesis of functionalized cyclopentenes and cyclohexenes with trialkylphosphines as nucleophilic catalysts Journal of the American Chemical Society 2002 124:2404-2405 DOI:10.1021/ja017123j PMID:11890766
- Roush, W. R., Limberakis, C., Kunz, R. K., Barda, D. A. Diastereoselective synthesis of the endo- and exo-spirotetronate subunits of the quartromicins. The first enantioselective Diels-Alder reaction of an acyclic (Z)-1,3-diene Organic Letters 2002 4:1543-1546 DOI:10.1021/ol025772+ PMID:11975624
- Roush, W. R., Barda, D. A. Partial stereochemical assignment of quartromicins A3 and D3 Organic Letters 2002 4:1539-1542 DOI:10.1021/ol025771h PMID:11975623
- Roush, W. R., Powell, N. A., James, R. A. Synthesis of structurally simplified aureolic acid aglycone-C-D-E trisaccharide analogues Australian Journal of Chemistry 2002 55:113-121 DOI:10.1071/ch01198
- Roush, W. R., James, R. A. Towards the synthesis of aureolic acid analogue conjugates: synthesis and glycosidation reactions of 3-O-acetyl-4-azido-2,4,6-trideoxy-L-glucopyranose derivatives Australian Journal of Chemistry 2002 55:141-146 DOI:10.1071/ch01199
- Caffrey, C. R., Hansell, E., Lucas, K. D., Brinen, L. S., Hernandez, A. A., Cheng, J. N., Gwaltney, S. L., Roush, W. R., Stierhof, Y. D., Bogyo, M., Steverding, D., McKerrow, J. H. Active site mapping, biochemical properties and subcellular localization of rhodesain, the major cysteine protease of Trypanosoma brucei rhodesiense Molecular and Biochemical Parasitology 2001 118:61-73 DOI:10.1016/s0166-6851(01)00368-1 PMID:11704274
- Roush, W. R., Madar, D. J., Coffey, D. S. Synthesis of highly functionalized naphthoate precursors to damavaricin D: observation of kinetically stable benzocyclohexadienones in the bromination reactions of highly functionalized beta-naphthol derivatives Canadian Journal of Chemistry-Revue Canadienne De Chimie 2001 79:1711-1726 DOI:10.1139/cjc-79-11-1711
- Roush, W. R., Cheng, J. M., Knapp-Reed, B., Alvarez-Hernandez, A., McKerrow, J. H., Hansell, E., Engel, J. C. Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain Bioorganic & Medicinal Chemistry Letters 2001 11:2759-2762 DOI:10.1016/s0960-894x(01)00566-2 PMID:11591518
- Roush, W. R., Bennett, C. E., Roberts, S. E. Studies on the synthesis of landomycin A: synthesis and glycosidation reactions of L-rhodinosyl acetate derivatives Journal of Organic Chemistry 2001 66:6389-6393 DOI:10.1021/jo015756a PMID:11559191
- Savall, B. M., Powell, N. A., Roush, W. R. Highly diastereoselective synthesis of propargylic 1,2-anti-diol derivatives using alpha-alkoxypropargylstannanes Organic Letters 2001 3:3057-3060 DOI:10.1021/ol016536m PMID:11554842
- Micalizio, G. C., Roush, W. R. Studies on the synthesis of pectenotoxin II: synthesis of a C(11)-C(26) fragment precursor via [3 + 2]-annulation reactions of chiral allylsilanes Organic Letters 2001 3:1949-1952 DOI:10.1021/ol0160250 PMID:11405752
- Menard, R., Therrien, C., Lachance, P., Sulea, T., Qi, H. T., Alvarez-Hernandez, A., Roush, W. R. Cathepsins X and B display distinct activity profiles that can be exploited for inhibitor design Biological Chemistry 2001 382:839-845 DOI:10.1515/bc.2001.102 PMID:11517939
- Yakelis, N. A., Roush, W. R. Lewis acid catalyzed intramolecular Diels-Alder reactions of acyclic (Z)-substituted 1,3-dienes Organic Letters 2001 3:957-960 DOI:10.1021/ol015667k PMID:11263925
- Therrien, C., Lachance, P., Sulea, T., Purisima, E. O., Qi, H. T., Ziomek, E., Alvarez-Hernandez, A., Roush, W. R., Menard, R. Cathepsins X and B can be differentiated through their respective mono- and dipeptidyl carboxypeptidase activities Biochemistry 2001 40:2702-2711 DOI:10.1021/bi002460a PMID:11258881
- Powell, N. A., Roush, W. R. Studies on the total synthesis of formamicin: synthesis of the C(1)-C(11) fragment Organic Letters 2001 3:453-456 DOI:10.1021/ol0069610 PMID:11428037
- Roush, W. R., Dilley, G. J. Studies on the synthesis of 2,6-disubstituted dihydropyrans: intervention of oxonia-Cope rearrangements in the Lewis acid mediated cyclodehydrative reactions of aldehydes and beta-hydroxyallylsilanes Synlett 2001 2001:955-959 DOI:10.1055/s-2001-14632
- Micalizio, G. C., Pinchuk, A. N., Roush, W. R. Synthesis of the C(29)-C(45) bis-pyran subunit (E-F) of spongistatin 1 (Altohyrtin A) Journal of Organic Chemistry 2000 65:8730-8736 DOI:10.1021/jo001236o PMID:11112596
- Roush, W. R., Hernandez, A. A., McKerrow, J. H., Selzer, P. M., Hansell, E., Engel, J. C. Design, synthesis and evaluation of D-homophenylalanyl epoxysuccinate inhibitors of the trypanosomal cysteine protease cruzain Tetrahedron 2000 56:9747-9762 DOI:10.1016/s0040-4020(00)00882-6
- Roush, W. R., Pinchuk, A. N., Micalizio, G. C. (E)-gamma-(dimethylphenylsilyl)allyl diisopinocampheylborane: a highly enantioselective reagent for the synthesis of anti-beta-hydroxyallylsilanes Tetrahedron Letters 2000 41:9413-9417 DOI:10.1016/s0040-4039(00)01526-4
- Frank, S. A., Chen, H., Kunz, R. K., Schnaderbeck, M. J., Roush, W. R. Use of thallium(I) ethoxide in Suzuki cross coupling reactions Organic Letters 2000 2:2691-2694 DOI:10.1021/ol0062446 PMID:10990429
- Brinen, L. S., Hansell, E., Cheng, J. M., Roush, W. R., McKerrow, J. H., Fletterick, R. J. A target within the target: probing cruzain's P1' site to define structural determinants for the Chagas' disease protease Structure with Folding & Design 2000 8:831-840 DOI:10.1016/s0969-2126(00)00173-8 PMID:10997902
- Roush, W. R., Bennett, C. E. A highly stereoselective synthesis of the landomycin A hexasaccharide unit Journal of the American Chemical Society 2000 122:6124-6125 DOI:10.1021/ja000743k
- Frank, S. A., Works, A. B., Roush, W. R. Studies on the synthesis of the decahydro-as-indacene ring system of (-)-spinosyn A via transannular Diels-Alder reactions of substituted (E,E,E)-cyclododeca-1,6,8-trienes Canadian Journal of Chemistry-Revue Canadienne De Chimie 2000 78:757-771 DOI:10.1139/cjc-78-6-757
- Roush, W. R., Pfeifer, L. A. Total synthesis of mycalamide A and 7-epi-mycalamide A Organic Letters 2000 2:859-862 DOI:10.1021/ol005629l PMID:10754688
- Micalizio, G. C., Roush, W. R. A three-component coupling strategy for tetrahydrofuran synthesis: application of the diisopropyl tartrate modified (E)-gamma-(dimethylphenylsilyl)allylboronate as an alpha,gamma-allyl dianion equivalent Organic Letters 2000 2:461-464 DOI:10.1021/ol9913082 PMID:10814351
- Roush, W. R., Gung, B. W., Bennett, C. E. 2-deoxy-2-iodo- and 2-deoxy-2-bromo-alpha-glucopyranosyl trichloroacetimidates: highly reactive and stereoselective donors for the synthesis of 2-deoxy-beta-glycosides Organic Letters 1999 1:891-893 DOI:10.1021/ol9908070 PMID:10823218
- Roush, W. R., Narayan, S. 2-deoxy-2-iodo-alpha-mannopyranosyl and -talopyranosyl acetates: highly stereoselective glycosyl donors for the synthesis of 2-deoxy-alpha-glycosides Organic Letters 1999 1:899-902 DOI:10.1021/ol9908068 PMID:10823220
- Roush, W. R., Narayan, S., Bennett, C. E., Briner, K. Iodoacetoxylation of glycals using cerium(IV) ammonium nitrate, sodium iodide, and acetic acid: stereoselective synthesis of 2-deoxy-2-iodo-alpha-mannopyranosyl acetates Organic Letters 1999 1:895-897 DOI:10.1021/ol990815g PMID:10823219
- Roush, W. R., Lane, G. C. Studies on the synthesis of tedanolide: synthesis of the C(5)-C(21) segment via a highly stereoselective fragment assembly aldol reaction of a chiral beta,gamma-unsaturated methyl ketone Organic Letters 1999 1:95-98 DOI:10.1021/ol990572s PMID:10822542
- Roush, W. R., Dilley, G. J. Studies of fragment assembly aldol reactions of chiral aldehydes and chiral methyl ketones: stereoselective synthesis of the C(13)-C(25) segment of scytophycin C Tetrahedron Letters 1999 40:4955-4959 DOI:10.1016/s0040-4039(99)00868-0
- Chemler, S. R., Roush, W. R. Stereochemically divergent pathways for the allylation and crotylation reactions of anti- and syn-beta-hydroxy-alpha-methyl aldehydes with allyl- and crotyltrifluorosilanes Tetrahedron Letters 1999 40:4643-4647 DOI:10.1016/s0040-4039(99)00730-3
- Micalizio, G. C., Roush, W. R. Towards the synthesis of spongistatin 1: diastereoselective synthesis of the C(36)-C(45) subunit Tetrahedron Letters 1999 40:3351-3354 DOI:10.1016/s0040-4039(99)00464-5
- Roush, W. R., Bennett, C. E. A highly stereoselective synthesis of 2-deoxy-beta-glycosides using 2-deoxy-2-iodo-glucopyranosyl acetate donors Journal of the American Chemical Society 1999 121:3541-3542 DOI:10.1021/ja984365j
- Chemler, S. R., Coffey, D. S., Roush, W. R. An improved synthesis of the (E,Z)-dienoate precursor of (+)-damavaricin D via a vinylogous Horner-Wadsworth-Emmons reaction Tetrahedron Letters 1999 40:1269-1272 DOI:10.1016/s0040-4039(98)02638-0
- Roush, W. R., Hernandez, A. A., Zepeda, G. A new synthesis of peptidyl epoxysuccinates for probing cysteine protease-inhibitor p-3/s-3 binding interactions Synthesis-Stuttgart 1999 1999:1500-1504 DOI:10.1055/s-1999-3648
- Scheidt, K. A., Tasaka, A., Bannister, T. D., Wendt, M. D., Roush, W. R. Total synthesis of (-)-bafilomycin A(1): application of diastereoselective crotylboration and methyl ketone aldol reactions Angewandte Chemie-International Edition 1999 38:1652-1655 DOI:10.1002/(sici)1521-3773(19990601)38:11<1652::aid-anie1652>3.0.co;2-k
- Roush, W. R., Hartz, R. A., Gustin, D. J. Total synthesis of olivomycin A Journal of the American Chemical Society 1999 121:1990-1991 DOI:10.1021/ja984229e
- Scheidt, K. A., Roush, W. R., McKerrow, J. H., Selzer, P. M., Hansell, E., Rosenthal, P. J. Structure-based design, synthesis and evaluation of conformationally constrained cysteine protease inhibitors Bioorganic & Medicinal Chemistry 1998 6:2477-2494 DOI:10.1016/s0968-0896(98)80022-9 PMID:9925304
- Roush, W. R., Gwaltney, S. L., Cheng, J. M., Scheidt, K. A., McKerrow, J. H., Hansell, E. Vinyl sulfonate esters and vinyl sulfonamides: potent, irreversible inhibitors of cysteine proteases Journal of the American Chemical Society 1998 120:10994-10995 DOI:10.1021/ja981792o
- Roush, W. R., Gonzalez, F. V., McKerrow, J. H., Hansell, E. Design and synthesis of dipeptidyl alpha',beta '-epoxy ketones, potent irreversible inhibitors of the cysteine protease cruzain Bioorganic & Medicinal Chemistry Letters 1998 8:2809-2812 DOI:10.1016/s0960-894x(98)00494-6 PMID:9873627
- Scheidt, K. A., Chen, H., Follows, B. C., Chemler, S. R., Coffey, D. S., Roush, W. R. Tris(dimethylamino)sulfonium difluorotrimethylsilicate, a mild reagent for the removal of silicon protecting groups Journal of Organic Chemistry 1998 63:6436-6437 DOI:10.1021/jo981215i
- Roush, W. R., Sciotti, R. J. Studies on the synthesis of chlorothricolide: diastereo- and enantioselective syntheses of model top-half spirotetronate units Journal of Organic Chemistry 1998 63:5473-5482 DOI:10.1021/jo980379w
- Roush, W. R., Sciotti, R. J. Enantioselective total synthesis of (-)-chlorothricolide via the tandem inter- and intramolecular Diels-Alder reaction of a hexaenoate intermediate Journal of the American Chemical Society 1998 120:7411-7419 DOI:10.1021/ja980611f
- Chemler, S. R., Roush, W. R. Concerning the synthesis of the elusive anti,anti-dipropionate stereotriad via the crotylation of beta-hydroxy alpha-methyl aldehydes with (Z)-crotyltrifluorosilane. Application to the synthesis of the C(7)-C(16) segment of zincophorin Journal of Organic Chemistry 1998 63:3800-3801 DOI:10.1021/jo980387c
- Roush, W. R., Pfeifer, L. A. Stereoselective N-acylation reactions of alpha-alkoxy carbamates Journal of Organic Chemistry 1998 63:2062-2063 DOI:10.1021/jo980024c
- Roush, W. R., Pfeifer, L. A., Marron, T. G. Studies on the synthesis of the mycalamides: Stereocontrolled synthesis of a model N-glycosylpederamide via a stereoselective aldol reaction Journal of Organic Chemistry 1998 63:2064-2065 DOI:10.1021/jo980023k
- Roush, W. R., Barda, D. A. An intramolecular Diels-Alder approach to the spirotetronic acid subunits of the quartromicins Tetrahedron Letters 1997 38:8781-8784 DOI:10.1016/s0040-4039(97)10415-4
- Roush, W. R., Barda, D. A. Second generation synthesis of the quartromicin spirotetronic acid subunits via a Claisen rearrangement intramolecular aldol sequence Tetrahedron Letters 1997 38:8785-8788 DOI:10.1016/s0040-4039(97)10416-6
- Roush, W. R., Reilly, M. L., Koyama, K., Brown, B. B. A formal total synthesis of (+)-tetronolide, the aglycon of the tetrocarcins: enantio- and diastereoselective syntheses of the octahydronaphthalene (bottom-half) and spirotetronate (top-half) fragments Journal of Organic Chemistry 1997 62:8708-8721 DOI:10.1021/jo970960c
- Roush, W. R., Coffey, D. S., Madar, D. J. Total synthesis of (+)-damavaricin D Journal of the American Chemical Society 1997 119:11331-11332 DOI:10.1021/ja971828x
- Roush, W. R., Barda, D. A. Highly selective Lewis acid catalyzed Diels-Alder reactions of acyclic (Z)-1,3-dienes Journal of the American Chemical Society 1997 119:7402-7403 DOI:10.1021/ja971070h
- Roush, W. R., Sebesta, D. P., Bennett, C. E. Stereoselective synthesis of 2-deoxy-beta-glycosides from glycal precursors. 1. Stereochemistry of the reactions of D-glucal derivatives with phenylsulfenyl chloride and phenylselenenyl chloride Tetrahedron 1997 53:8825-8836 DOI:10.1016/s0040-4020(97)90394-x
- Roush, W. R., Sebesta, D. P., James, R. A. Stereoselective synthesis of 2-deoxy-beta-glycosides from glycal precursors. 2. Stereochemistry of glycosidation reactions of 2-thiophenyl- and 2-selenophenyl-alpha-D-gluco-pyranosyl donors Tetrahedron 1997 53:8837-8852 DOI:10.1016/s0040-4020(97)00572-3
- Hunt, J. A., Roush, W. R. 4,5-diisopropyl-B-[(E)-[(3'-menthofuryl)dimethylsilyl]allyl]-1,3,2-dioxaborolane, an improved chiral reagent for the anti alpha-hydroxyallylation of aldehydes: application to the enantioselective synthesis of (-)-swainsonine Journal of Organic Chemistry 1997 62:1112-1124 DOI:10.1021/jo961840s
- Roush, W. R., Marron, T. G., Pfeifer, L. A. Highly diastereoselective synthesis of pederic acid derivatives Journal of Organic Chemistry 1997 62:474-478 DOI:10.1021/jo961841k PMID:11671436
- Roush, W. R., Works, A. B. Diastereofacially selective enolate Claisen rearrangements of 4-7-eta 4-(1-acyloxy-2,4,6-octatrienyl) tricarbonyliron complexes Tetrahedron Letters 1997 38:351-354 DOI:10.1016/s0040-4039(96)02349-0
- Roush, W. R., Champoux, J. A., Peterson, B. C. Diastereoselective synthesis of the cis-octahydronaphthalene nucleus of superstolides A and B Tetrahedron Letters 1996 37:8989-8992 DOI:10.1016/s0040-4039(96)02110-7
- Roush, W. R., Works, A. B. Diastereoselective synthesis of the trans-anti-cis-decahydro-as-indacene ring system via the transannular Diels-Alder reaction of a functionalized (E,E,E)-cyclododeca-1,6,8-triene Tetrahedron Letters 1996 37:8065-8068 DOI:10.1016/0040-4039(96)01840-0
- Hunt, J. A., Roush, W. R. Solid-phase synthesis of 6-deoxyoligosaccharides Journal of the American Chemical Society 1996 118:9998-9999 DOI:10.1021/ja962128f
- Roush, W. R., Briner, K., Kesler, B. S., Murphy, M., Gustin, D. J. Studies on the synthesis of aureolic acid antibiotics: acyloin glycosidation studies Journal of Organic Chemistry 1996 61:6098-6099 DOI:10.1021/jo960932e PMID:11667440
- Roush, W. R., Coffey, D. S., Madar, D., Palkowitz, A. D. Studies on the synthesis of the streptovaricins: total synthesis of 24,27-dimethyl dihydrodamavaricin D Journal of the Brazilian Chemical Society 1996 7:327-334
- Roush, W. R., Koyama, K., Curtin, M. L., Moriarty, K. J. Studies on the synthesis of nargenicin A(1): highly stereoselective synthesis of the complete carbon framework via the transannular Diels-Alder reaction of an 18-membered macrolide Journal of the American Chemical Society 1996 118:7502-7512 DOI:10.1021/ja9607796
- Roush, W. R., Coffey, D. S. Synthesis of the naphthoquinone nucleus of awamycin Journal of Organic Chemistry 1995 60:4412-4418 DOI:10.1021/jo00119a018
- Gustin, D. J., Vannieuwenhze, M. S., Roush, W. R. Diastereoselective aldol reactions of chiral aldehydes and chiral methyl ketones: dependence of stereoselectivity on the metal enolate, the aldehyde 2,3-stereochemistry, and the aldehyde β-alkoxy protecting group Tetrahedron Letters 1995 36:3443-3446 DOI:10.1016/0040-4039(95)00626-n
- Gustin, D. J., Vannieuwenhze, M. S., Roush, W. R. Synthesis of the C(3)-C(15) segment of rutamycin B via a C(8)-C(9) fragment assembly aldol reaction: metal dependence of the aldehyde and enolate diastereofacial selectivities Tetrahedron Letters 1995 36:3447-3450 DOI:10.1016/0040-4039(95)00628-p
- Marron, T. G., Roush, W. R. Diastereoselective synthesis of N-benzoyl mycalamine, the fully elaborated trioxadecalin nucleus of mycalamide. A. Control of the key N-acyl aminal stereocenter via carbamate acylation Tetrahedron Letters 1995 36:1581-1584 DOI:10.1016/0040-4039(95)00093-r
- Roush, W. R., Lin, X. F. Studies on the synthesis of aureolic acid antibiotics: highly stereoselective synthesis of aryl 2-deoxy-beta-glycosides via the Mitsunobu reaction and synthesis of the olivomycin A-B disaccharide Journal of the American Chemical Society 1995 117:2236-2250 DOI:10.1021/ja00113a013
- Hunt, J. A., Roush, W. R. Diisopropyl tartrate-modified (E)-γ-[(menthofuryl)dimethylsilyl]-allyl boronate, an improved chiral reagent for the anti α-hydroxyallylation of aldehydes. Application to the enantioselective synthesis of (−)-swainsonine Tetrahedron Letters 1995 36:501-504 DOI:10.1016/0040-4039(94)02295-m
- Roush, W. R., Hunt, J. A. Asymmetric allylboration of 2-N,3-O-isopropylidene-N-boc-L-serinal: diastereoselective synthesis of the calicheamicin gamma1I amino sugar Journal of Organic Chemistry 1995 60:798-806 DOI:10.1021/jo00109a008
- Roush, W. R., Grover, P. T. N,N'-bis(2,2,2-trifluoroethyl)-N,N'-ethylenetartramide: an improved chiral auxiliary for the asymmetric allylboration reaction Journal of Organic Chemistry 1995 60:3806-3813 DOI:10.1021/jo00117a036
- Wada, C. K., Roush, W. R. Highly stereoselective 1,4-addition reactions of alkylidene malonate substituted η4-(1,3-butadienyl)iron(tricarbonyl) complexes Tetrahedron Letters 1994 35:7351-7354 DOI:10.1016/0040-4039(94)85311-8
- Roush, W. R., Wada, C. K. Highly stereoselective substitution reactions of functionalized η4-[3(E),5(E)-heptadien-2-ol]iron tricarbonyl complexes Tetrahedron Letters 1994 35:7347-7350 DOI:10.1016/0040-4039(94)85310-x
- Roush, W. R., Vannieuwenhze, M. S. [(Z)-gamma-[(Diisopropylidene-alpha-D-mannopyranosyl)oxy]allyl]tributylstannane: a new chiral reagent for the asymmetric alpha-hydroxyallylation of aldehydes Journal of the American Chemical Society 1994 116:8536-8543 DOI:10.1021/ja00098a014
- Li, Z., Chen, X., Davidson, E., Zwang, O., Mendis, C., Ring, C. S., Roush, W. R., Fegley, G., Li, R., Rosenthal, P. J., Lee, G. K., Kenyon, G. L., et al. Anti-malarial drug development using models of enzyme structure Chemistry & Biology 1994 1:31-37 DOI:10.1016/1074-5521(94)90038-8 PMID:9383368
- Roush, W. R., Sciotti, R. J. Enantioselective total synthesis of (-)-chlorothricolide Journal of the American Chemical Society 1994 116:6457-6458 DOI:10.1021/ja00093a065
- Roush, W. R., Gustin, D. A stereochemically general synthesis of methyl 2,4,6-trideoxy-4-methylthio-α-D-ribo-pyranoside, the thio sugar of esperamicin A(1) Tetrahedron Letters 1994 35:4931-4934 DOI:10.1016/s0040-4039(00)73285-0
- Roush, W. R., Follows, B. C. Asymmetric synthesis of the hydroxylamino sugar of calicheamicin Tetrahedron Letters 1994 35:4935-4938 DOI:10.1016/s0040-4039(00)73286-2
- Roush, W. R., Wada, C. K. Application of eta4-diene iron tricarbonyl complexes in acyclic stereocontrol: asymmetric synthesis of the as-indacene unit of ikarugamycin (a formal total synthesis) Journal of the American Chemical Society 1994 116:2151-2152 DOI:10.1021/ja00084a068
- Roush, W. R., Grover, P. T., Marron, T. G. Allylboronates in organic synthesis: design of an improved chiral auxiliary and synthesis of the trioxadecalin nucleus of mycalamides A and B Special publication (Royal Society of Chemistry (Great Britain)) 1994 143:113-118
- Roush, W. R., Bannister, T. D., Wendt, M. D. Concerning the diastereofacial selectivity of aldol reactions of chiral methyl ketone enolates: evidence for remote chelation in the bafilomycin aldol reaction Tetrahedron Letters 1993 34:8387-8390 DOI:10.1016/s0040-4039(00)61340-0
- Roush, W. R., Lin, X. F. Synthesis of naphthyl A–B disaccharides corresponding to olivomycin A and mithramycin Tetrahedron Letters 1993 34:6829-6832 DOI:10.1016/s0040-4039(00)91806-9
- Roush, W. R., Warmus, J. S., Works, A. B. Synthesis and transannular diels-alder reactions of (E,E,E)-cyclotetradeca-2,8,10-trienones Tetrahedron Letters 1993 34:4427-4430 DOI:10.1016/0040-4039(93)88050-s
- Roush, W. R., Brown, B. B. A highly diastereoselective and enantioselective synthesis of the top half of kijanolide Journal of Organic Chemistry 1993 58:2151-2161 DOI:10.1021/jo00060a035
- Roush, W. R., Brown, B. B. Studies on the synthesis of kijanolide: synthesis of the 2-acyl spiro tetronate and investigations concerning the coupling of the top and bottom half fragments Journal of Organic Chemistry 1993 58:2162-2172 DOI:10.1021/jo00060a036
- Roush, W. R., Briner, K., Sebesta, D. P. Highly stereoselective synthesis of alpha-L-olivomycosides via trimethylsilyl triflate mediated glycosidations of 1-O-acetyl-4-O-isobutyryl-2,6-dideoxy-2-iodo-3-C-methyl-alpha-L-mannopyranose Synlett 1993 1993:264-266 DOI:10.1055/s-1993-22425
- Roush, W. R., Brown, B. B. Application of the steric directing group strategy to the stereoselective synthesis of the octahydronaphthalene substructure of kijanolide and tetronolide Journal of the American Chemical Society 1993 115:2268-2278 DOI:10.1021/ja00059a024
- Roush, W. R., Madar, D. J. Towards the synthesis of streptovaricin D: synthesis of fully elaborated aromatic precursors and coupling with ansa chain fragments Tetrahedron Letters 1993 34:1553-1556 DOI:10.1016/0040-4039(93)85004-g
- Roush, W. R., Marron, T. G. Toward the synthesis of mycalamides A, B and onnamide A: a highly stereoselective synthesis of the trioxadecalin ring system Tetrahedron Letters 1993 34:5421-5424 DOI:10.1016/s0040-4039(00)73924-4
- Roush, W. R., Murphy, M. An improved synthesis of naphthoate precursors to olivin Journal of Organic Chemistry 1992 57:6622-6629 DOI:10.1021/jo00050a047
- Roush, W. R., Koyama, K. Enantioselective synthesis of the top half of tetronolide Tetrahedron Letters 1992 33:6227-6230 DOI:10.1016/s0040-4039(00)60939-5
- Sebesta, D. P., Roush, W. R. Synthesis of C-D-E trisaccharide precursors of olivomycin A Journal of Organic Chemistry 1992 57:4799-4802 DOI:10.1021/jo00044a010
- Roush, W. R., Sciotti, R. J. Enantioselective synthesis of the top half of chlorothricolide Tetrahedron Letters 1992 33:4691-4694 DOI:10.1016/s0040-4039(00)61260-1
- Roush, W. R., Bannister, T. D. Stereoselective synthesis of the C(13)-C(25) segment of bafilomycin A(1) Tetrahedron Letters 1992 33:3587-3590 DOI:10.1016/s0040-4039(00)92509-7
- Roush, W. R., Brown, B. B. Enantioselective synthesis of 2-alkyl-5-methylene-1,3-dioxolan-4-ones and exo-selective Diels-Alder reactions with cyclopentadiene Journal of Organic Chemistry 1992 57:3380-3387 DOI:10.1021/jo00038a028
- Roush, W. R., Ratz, A. M., Jablonowski, J. A. Solid-state and solution conformational-analysis of tartrate-derived 1,3-dioxolanes and 1,3,2-dioxaborolanes Journal of Organic Chemistry 1992 57:2047-2052 DOI:10.1021/jo00033a027
- Roush, W. R., Grover, P. T. Diisopropyl tartrate modified (E)-γ-[(cyclohexyloxy)dimethylsilyl]- and (E)-γ-(dimethylphenylsilyl)allylboronates: chiral reagents for the enantio- and diastereoselective synthesis of anti 1,2-diols and 2-butene-1,4-diols via the formal α- and γ-hydroxyallylation of aldehydes Tetrahedron 1992 48:1981-1998 DOI:10.1016/s0040-4020(01)88869-4
- Roush, W. R., Park, J. C. Asymmetric allylborations of 3-decynal dicobalt hexacarbonyl: cobalt induced reversal of enantioselectivity and applications to highly diastereoselective intramolecular Pauson-Khand reactions Tetrahedron Letters 1991 32:6285-6288 DOI:10.1016/0040-4039(91)80148-y
- Roush, W. R., Lin, X. F. A highly stereoselective synthesis of aryl 2-deoxy-beta-glycosides via the Mitsunobu reaction Journal of Organic Chemistry 1991 56:5740-5742 DOI:10.1021/jo00020a003
- Roush, W. R. Concerning the diastereofacial selectivity of the aldol reactions of alpha-methyl chiral aldehydes and lithium and boron propionate enolates Journal of Organic Chemistry 1991 56:4151-4157 DOI:10.1021/jo00013a015
- Roush, W. R., Lin, X. F., Straub, J. A. A highly stereoselective synthesis of the AB disaccharide unit of olivomycin A Journal of Organic Chemistry 1991 56:1649-1655 DOI:10.1021/jo00004a054
- Roush, W. R., Straub, J. A., Vannieuwenhze, M. S. A stereochemically general synthesis of 2-deoxyhexoses via the asymmetric allylboration of 2,3-epoxyaldehydes Journal of Organic Chemistry 1991 56:1636-1648 DOI:10.1021/jo00004a053
- Roush, W. R., Kageyama, M., Riva, R., Brown, B. B., Warmus, J. S., Moriarty, K. J. Enantioselective synthesis of the bottom half of chlorothricolide. 3. Studies of the steric directing group strategy for stereocontrol in intramolecular Diels-Alder reactions Journal of Organic Chemistry 1991 56:1192-1210 DOI:10.1021/jo00003a049
- Roush, W. R., Palkowitz, A. D., Ando, K. Acyclic diastereoselective synthesis using tartrate ester modified crotylboronates: double asymmetric reactions with alpha-methyl chiral aldehydes and synthesis of the C19-C29 segment of rifamycin S Journal of the American Chemical Society 1990 112:6348-6359 DOI:10.1021/ja00173a024
- Roush, W. R., Ando, K., Powers, D. B., Palkowitz, A. D., Halterman, R. L. Asymmetric-synthesis using diisopropyl tartrate modified (E)-crotylboronates and (Z)-crotylboronates: preparation of the chiral crotylboronates and reactions with achiral aldehydes Journal of the American Chemical Society 1990 112:6339-6348 DOI:10.1021/ja00173a023
- Roush, W. R., Hoong, L. K., Palmer, M. A. J., Straub, J. A., Palkowitz, A. D. Asymmetric synthesis using tartrate ester modified allylboronates. 2. Single and double asymmetric reactions with alkoxy-substituted aldehydes Journal of Organic Chemistry 1990 55:4117-4126 DOI:10.1021/jo00300a032
- Roush, W. R., Hoong, L. K., Palmer, M. A. J., Park, J. C. Asymmetric synthesis using tartrate ester modified allylboronates.1. Factors influencing stereoselectivity Journal of Organic Chemistry 1990 55:4109-4117 DOI:10.1021/jo00300a031
- Roush, W. R., Park, J. C. Use of metal carbonyl complexes to achieve high enantioselectivity in the asymmetric allylboration of unsaturated aldehydes Journal of Organic Chemistry 1990 55:1143-1144 DOI:10.1021/jo00291a009
- Roush, W. R., Park, J. C. Asymmetric allylborations of diene aldehyde Fe(CO)3 derivatives: efficient kinetic resolution of racemic complexes and the highly enantiotopic group and face selective allylboration of a meso substrate Tetrahedron Letters 1990 31:4707-4710 DOI:10.1016/s0040-4039(00)97712-8
- Roush, W. R., Grover, P. T. Diisopropyl tartrate (E)-γ-(dimethylphenylsilyl)allylboronate, a chiral allylic alcohol β-carbanion equivalent for the enantioselective synthesis of 2-butene-1,4-diols from aldehydes Tetrahedron Letters 1990 31:7567-7570 DOI:10.1016/s0040-4039(00)97300-3
- Roush, W. R., Grover, P. T., Lin, X. F. Diisopropyl tartrate modified (E)-γ-[(cyclohexyloxy)dimethylsilyl-allylboronate, a chiral reagent for the stereoselective synthesis of anti 1,2-diols via the formal α-hydroxyallylation of aldehydes Tetrahedron Letters 1990 31:7563-7566 DOI:10.1016/s0040-4039(00)97299-x
- Roush, W. R. Stereochemical and synthetic studies of the intramolecular Diels-Alder reaction Advances in Cycloaddition 1990 2:91-146
- Roush, W. R., Moriarty, K. J., Brown, B. B. Stereoselective synthesis of (Z,E)-2-bromo-1,3-dienes via the palladium (O) catalyzed cross coupling reactions of 1,1-dibromoolefins and vinylboronic acids Tetrahedron Letters 1990 31:6509-6512 DOI:10.1016/s0040-4039(00)97103-x
- Roush, W. R., Palkowitz, A. D. Synthesis of the C(1)-C(15) segment of streptovaricin D Journal of Organic Chemistry 1989 54:3009-3011 DOI:10.1021/jo00274a008
- Roush, W. R., Michaelides, M. R., Tai, D. F., Lesur, B. M., Chong, W. K. M., Harris, D. J. A highly stereoselective synthesis of (+)-olivin, the aglycon of olivomycin A Journal of the American Chemical Society 1989 111:2984-2995 DOI:10.1021/ja00190a036
- Coe, J. W., Roush, W. R. Studies of an intramolecular Diels-Alder approach to the nargenicins: involvement of boatlike transition states in the cyclizations of substituted 1,7,9-decatrien-3-ones Journal of Organic Chemistry 1989 54:915-930 DOI:10.1021/jo00265a036
- Roush, W. R. Applications of allylboronates in the synthesis of carbohydrates and polyhydroxylated natural products ACS Symposium Series 1989 386:242-277 DOI:10.1021/bk-1989-0386.ch014
- Roush, W. R., Brown, B. B. Diastereoselective synthesis of the top half of kijanolide Tetrahedron Letters 1989 30:7309-7312 DOI:10.1016/s0040-4039(00)70684-8
- Roush, W. R. Evolution of a strategy for the synthesis of olivomycin A: development of methodology for the diastereo- and enantioselective synthesis of carbohydrates from acyclic precursors Strategies and Tactics in Organic Synthesis 1989 323-367
- Roush, W. R., Essenfeld, A. P., Warmus, J. S., Brown, B. B. Synthesis and Diels-Alder reactions of 2-alkyl-5-methylene-1,3-dioxolan-4-ones and 2-alkyl-3-acyl-5-methylene-1,3-oxazolidin-4-ones: highly exo and diastereoface selective chiral ketene equivalents Tetrahedron Letters 1989 30:7305-7308 DOI:10.1016/s0040-4039(00)70683-6
- Roush, W. R., Banfi, L., Park, J. C., Hoong, L. K. The asymmetric allylboration reaction: dependence of rate and enantioselectivity on the chiral auxiliary Tetrahedron Letters 1989 30:6457-6460 DOI:10.1016/s0040-4039(01)88993-0
- Roush, W. R., Banfi, L. N,N'-dibenzyl-N,N'-ethylenetartramide: a rationally designed chiral auxiliary for the allylboration reaction Journal of the American Chemical Society 1988 110:3979-3982 DOI:10.1021/ja00220a041
- Roush, W. R., Riva, R. Enantioselective synthesis of the bottom half of chlorothricolide. 2. A comparative study of substituent effects on the stereoselectivity of the key intramolecular Diels-Alder reaction Journal of Organic Chemistry 1988 53:710-712 DOI:10.1021/jo00238a049
- Roush, W. R., Brown, B. B., Drozda, S. E. A highly stereoselective synthesis of the octahydronaphthalene subunit of kijanolide and tetronolide Tetrahedron Letters 1988 29:3541-3544 DOI:10.1016/0040-4039(88)85287-0
- Roush, W. R., Ando, K., Powers, D. B., Halterman, R. L., Palkowitz, A. D. Enantioselective synthesis using diisopropyl tartrate modified (E)- and (Z)-crotylboronates: reactions with achiral aldehydes Tetrahedron Letters 1988 29:5579-5582 DOI:10.1016/s0040-4039(00)80816-3
- Roush, W. R., Michaelides, M. R., Tai, D. F., Chong, W. K. M. A highly stereoselective total synthesis of the natural enantiomer of olivin Journal of the American Chemical Society 1987 109:7575-7577 DOI:10.1021/ja00258a077
- Halterman, R. L., Roush, W. R., Hoong, L. K. Analytical resolution of secondary methyl ethers by chiral complexation gas chromatography Journal of Organic Chemistry 1987 52:1152-1155 DOI:10.1021/jo00382a036
- Roush, W. R., Palkowitz, A. D. Applications of tartrate ester modified allylic boronates in organic-synthesis: an efficient, highly stereoselective synthesis of the C19-C29 segment of rifamycin S Journal of the American Chemical Society 1987 109:953-955 DOI:10.1021/ja00237a082
- Roush, W. R., Palkowitz, A. D., Palmer, M. A. J. Reactions of diisopropyl tartrate modified allyl- and (E)- and (Z)-crotylboronates with beta-alkoxy-alpha-methylpropionaldehydes: a reagent-based solution to the acyclic dipropionate problem Journal of Organic Chemistry 1987 52:316-318 DOI:10.1021/jo00378a041
- Roush, W. R., Essenfeld, A. P., Warmus, J. S. Effect of dienophile activating group on the stereoselectivity of the intramolecular Diels-Alder reaction Tetrahedron Letters 1987 28:2447-2450 DOI:10.1016/s0040-4039(00)95437-6
- Roush, W. R., Coe, J. W. Studies on the synthesis of nargenicin A(1). An example of anintramolecular Diels-Alder reaction that proceeds with a boat-likeconformation of the connecting chain Tetrahedron Letters 1987 28:931-934 DOI:10.1016/s0040-4039(00)95877-5
- Roush, W. R., Straub, J. A., Brown, R. J. Total synthesis of carbohydrates. 5. Stereochemistry of the epoxidations of acyclic allylic amides. Applications towards the synthesis of 2,3,6-trideoxy-3-aminohexoses Journal of Organic Chemistry 1987 52:5127-5136 DOI:10.1021/jo00232a014
- Roush, W. R., Russorodriguez, S. Trichothecene degradation studies. 2. Synthesis of [13-(14)-C] anguidine Journal of Organic Chemistry 1987 52:598-603 DOI:10.1021/jo00380a021
- Roush, W. R., Russorodriguez, S. Trichothecene degradation studies. 3. Synthesis of 12,13-deoxy-12,13-methanoanguidine and 12-epianguidine, two optically active analogs of the epoxytrichothecene mycotoxin anguidine Journal of Organic Chemistry 1987 52:603-606 DOI:10.1021/jo00380a022
- Roush, W. R., Adam, M. A., Walts, A. E., Harris, D. J. Stereochemistry of the reactions of substituted allylboronates with chiral aldehydes: factors influencing aldehyde diastereofacial selectivity Journal of the American Chemical Society 1986 108:3422-3434 DOI:10.1021/ja00272a043
- Roush, W. R., Halterman, R. L. Diisopropyl tartrate modified (E)-crotylboronates: highly enantioselective propionate (E)-enolate equivalents Journal of the American Chemical Society 1986 108:294-296 DOI:10.1021/ja00262a018
- Roush, W. R., Michaelides, M. R. Studies on the total synthesis of sesbanimide: highly diastereoselective synthesis of the AB ring system Tetrahedron Letters 1986 27:3353-3356 DOI:10.1016/s0040-4039(00)84794-2
- Roush, W. R., Straub, J. A. Total synthesis of the AB disaccharide unit of olivomycin A Tetrahedron Letters 1986 27:3349-3352 DOI:10.1016/s0040-4039(00)84793-0
- Roush, W. R., Russorodriguez, S. Trichothecene degradation studies: synthesis of 12,13-deoxyanguidine and 12,13-deoxyverrucarol Journal of Organic Chemistry 1985 50:5465-5468 DOI:10.1021/jo00350a004
- Roush, W. R., Walts, A. E., Hoong, L. K. Diastereoselective and enantioselective aldehyde addition-reactions of 2-allyl-1,3,2-dioxaborolane-4,5-dicarboxylic esters, a useful class of tartrate ester modified allylboronates Journal of the American Chemical Society 1985 107:8186-8190 DOI:10.1021/ja00312a062
- Walts, A. E., Roush, W. R. A stereorational total synthesis of (-)-ptilocaulin Tetrahedron 1985 41:3463-3478 DOI:10.1016/s0040-4020(01)96701-8
- Roush, W. R., Adam, M. A. Directed openings of 2,3-epoxy alcohols via reactions with isocyanates: synthesis of (+)-erythro-dihydrosphingosine Journal of Organic Chemistry 1985 50:3752-3757 DOI:10.1021/jo00220a015
- Roush, W. R., Kageyama, M. Enantioselective synthesis of the bottom half of chlorothricolide Tetrahedron Letters 1985 26:4327-4330 DOI:10.1016/s0040-4039(00)98725-2
- Roush, W. R., Adam, M. A., Harris, D. J. Stereochemistry of crotylboronate additions to alpha,beta-dialkoxy aldehydes Journal of Organic Chemistry 1985 50:2000-2003 DOI:10.1021/jo00211a051
- Roush, W. R., Walts, A. E. Stereochemistry of the reactions of pinacol allylboronate with two α,β-dialkoxyaldehydes Tetrahedron Letters 1985 26:3427-3430 DOI:10.1016/s0040-4039(00)98655-6
- Roush, W. R., Russorodriguez, S. Synthesis of 4-beta-acetoxyscirpene-3-alpha,15-diol Journal of Organic Chemistry 1985 50:3224-3226 DOI:10.1021/jo00217a046
- Roush, W. R., Hagadorn, S. M. Synthesis of mycarose and epi-axenose from non-carbohydrate precursors Carbohydrate Research 1985 136:187-193 DOI:10.1016/0008-6215(85)85195-8 PMID:4005889
- Roush, W. R., Marletta, M. A., Russo-Rodriguez, S., Recchia, J. Trichothecene metabolism studies. 2. Structure of 3α-(1'β-D-glucopyranosiduronyl)-8α-isovaleryloxyscirpen-3,4β,15-triol 15-acetate produced from T-2 toxin in vitro Tetrahedron Letters 1985 26:5231-5234 DOI:10.1016/S0040-4039(00)95002-0
- Roush, W. R., Marletta, M. A., Russo-Rodriguez, S., Recchia, J. Trichothecene metabolism studies: isolation and structure determination of 15-acetyl-3α-(1'β-D-glucopyranosiduronyl)scirpen-3,4β,15-triol Journal of the American Chemical Society 1985 107:3354-3355 DOI:10.1021/ja00297a055
- Blanchette, M. A., Choy, W., Davis, J. T., Essenfeld, A. P., Masamune, S., Roush, W. R., Sakai, T. Horner-Wadsworth-Emmons reaction: use of lithium chloride and an amine for base-sensitive compounds Tetrahedron Letters 1984 25:2183-2186 DOI:10.1016/s0040-4039(01)80205-7
- Roush, W. R., Gillis, H. R., Essenfeld, A. P. Hydrofluoric acid catalyzed intramolecular Diels-Alder reactions Journal of Organic Chemistry 1984 49:4674-4682 DOI:10.1021/jo00198a018
- Roush, W. R., Peseckis, S. M., Walts, A. E. Synthesis of antibiotic X-14547A Journal of Organic Chemistry 1984 49:3429-3432 DOI:10.1021/jo00192a052
- Roush, W. R., Blizzard, T. A. Synthesis of epoxytrichothecenes: verrucarin J and verrucarin J isomers Journal of Organic Chemistry 1984 49:1772-1783 DOI:10.1021/jo00184a021
- Roush, W. R., Blizzard, T. A. Synthesis of verrucarin B Journal of Organic Chemistry 1984 49:4332-4339 DOI:10.1021/jo00197a002
- Roush, W. R., Walts, A. E. Total synthesis of (-)-ptilocaulin Journal of the American Chemical Society 1984 106:721-723 DOI:10.1021/ja00315a044
- Roush, W. R., Adam, M. A., Peseckis, S. M. Regioselectivity of the reactions of trialkylaluminum reagents with 2,3-epoxyalcohols: application to the synthesis of α-chiral aldehydes Tetrahedron Letters 1983 24:1377-1380 DOI:10.1016/s0040-4039(00)81660-3
- Roush, W. R., Lesur, B. M. Stereochemistry of vinyl cuprate additions to carbohydrate-derived enones and α,β-unsaturated esters Tetrahedron Letters 1983 24:2231-2234 DOI:10.1016/s0040-4039(00)81891-2
- Roush, W. R., Harris, D. J., Lesur, B. M. Studies on the synthesis of olivin: diastereoselective synthesis of a functionalized D-fucose derivative Tetrahedron Letters 1983 24:2227-2230 DOI:10.1016/s0040-4039(00)81890-0
- Roush, W. R., Spada, A. P. Synthesis of trichoverrol B Tetrahedron Letters 1983 24:3693-3696 DOI:10.1016/s0040-4039(00)94511-8
- Roush, W. R., Blizzard, T. A. Synthesis of verrucarin J Journal of Organic Chemistry 1983 48:758-759 DOI:10.1021/jo00153a035
- Roush, W. R., Dambra, T. E. Total synthesis of (+/-)-verrucarol Journal of the American Chemical Society 1983 105:1058-1060 DOI:10.1021/ja00342a071
- Roush, W. R., Brown, R. J., Dimare, M. Total synthesis of carbohydrates. 2. Regiochemical control of nucleophilic ring opening of acylated 2,3-epoxy alcohols Journal of Organic Chemistry 1983 48:5083-5093 DOI:10.1021/jo00173a056
- Roush, W. R., Brown, R. J. Total synthesis of carbohydrates. 3. Efficient enantioselective syntheses of 2,6-dideoxyhexoses Journal of Organic Chemistry 1983 48:5093-5101 DOI:10.1021/jo00173a057
- Roush, W. R., Spada, A. P. Enantioselective and stereoselective syntheses of the dihydroxyoctadienoic acid fragments of the roridins and trichoverrins Tetrahedron Letters 1982 23:3773-3776 DOI:10.1016/s0040-4039(00)87703-5
- Roush, W. R., Gillis, H. R. Further stereochemical aspects of intramolecular Diels-Ader reactions in the undeca-2,8,10-trienoate ester series Journal of Organic Chemistry 1982 47:4825-4829 DOI:10.1021/jo00146a001
- Roush, W. R., Blizzard, T. A., Basha, F. Z. Methodology for the synthesis of the acyclic portions of verrucarins A and J Tetrahedron Letters 1982 23:2331-2334 DOI:10.1016/s0040-4039(00)87334-7
- Roush, W. R., Gillis, H. R., Ko, A. I. Stereochemical aspects of the intramolecular Diels-Alder reactions of deca-2,7,9-trienoate esters. 3. Thermal, Lewis acid-catalyzed, and asymmetric cyclizations Journal of the American Chemical Society 1982 104:2269-2283 DOI:10.1021/ja00372a027
- Roush, W. R., Peseckis, S. M. Studies on the total synthesis of antibiotic X-14547A: the pentaene approach Tetrahedron Letters 1982 23:4879-4882 DOI:10.1016/s0040-4039(00)85737-8
- Hall, S. E., Roush, W. R. Synthesis of the bottom half of chlorothricolide Journal of Organic Chemistry 1982 47:4611-4621 DOI:10.1021/jo00145a002
- Roush, W. R., Brown, R. J. Total synthesis of carbohydrates: stereoselective syntheses of 2,6-dideoxy-D-arabino-hexose and 2,6-dideoxy-D-ribo-hexose Journal of Organic Chemistry 1982 47:1371-1373 DOI:10.1021/jo00346a050
- Roush, W. R., Myers, A. G. Antibiotic X-14547A: total synthesis of the right-hand half Journal of Organic Chemistry 1981 46:1509-1511 DOI:10.1021/jo00320a060
- Roush, W. R., Peseckis, S. M. Intramolecular Diels-Alder reactions: the angularly methylated trans-perhydroindan ring system Journal of the American Chemical Society 1981 103:6696-6704 DOI:10.1021/ja00412a027
- Roush, W. R., Hall, S. E. Studies on the total synthesis of chlorothricolide: stereochemical aspects of the intramolecular Diels-Alder reactions of methyl undeca-2,8,10-trienoates Journal of the American Chemical Society 1981 103:5200-5211 DOI:10.1021/ja00407a042
- Roush, W. R., Dambra, T. E. Synthesis of a bicyclic precursor to verrucarol: application of a trimethylsilyl-controlled Diels-Alder reaction and Wagner-Meerwein rearrangement sequence Journal of Organic Chemistry 1981 46:5045-5047 DOI:10.1021/jo00337a059
- Roush, W. R., Gillis, H. R. Improved synthesis of the perhydroindenone precursor of dendrobine Journal of Organic Chemistry 1980 45:4283-4287 DOI:10.1021/jo01310a006
- Roush, W. R., Ko, A. I., Gillis, H. R. Stereochemical aspects of the intramolecular Diels-Alder reactions of methyl deca-2,7,9-trienoates. 1. Thermal cyclizations Journal of Organic Chemistry 1980 45:4264-4267 DOI:10.1021/jo01309a054
- Roush, W. R., Gillis, H. R., Hall, S. E. Stereoselective syntheses of substituted methyl (Z,E,E)-deca-2,7.9-trienoates and substituted methyl (Z,E,E)-undeca-2,8,10-trienoates Tetrahedron Letters 1980 21:1023-1026 DOI:10.1016/s0040-4039(00)78829-0
- Roush, W. R. Total synthesis of (+/-)-dendrobine Journal of the American Chemical Society 1980 102:1390-1404 DOI:10.1021/ja00524a027
- Roush, W. R., Dambra, T. E. Total synthesis of verrucarol: a stereoselective synthesis of 13,14-dinor-15-hydroxytrichothec-9-ene Journal of Organic Chemistry 1980 45:3927-3929 DOI:10.1021/jo01307a045
- Roush, W. R. Stereochemical aspects of the intramolecular Diels-Alder reactions of methyl (E,E,E)- and (Z,E,E)-6-alkoxy-11-methyldodeca-2,7,9-trienoate Journal of Organic Chemistry 1979 44:4008-4010 DOI:10.1021/jo01336a067
- Roush, W. R. Total synthesis of (+/-)-dendrobine Journal of the American Chemical Society 1978 100:3599-3601 DOI:10.1021/ja00479a053
- Roush, W. R., Feitler, D., Rebek, J. Polymer-bound tosyl azide Tetrahedron Letters 1974 1391-1392 DOI:10.1016/S0040-4039(01)82499-0
chapter
- Nanna, A. R., Roush, W. R., Rader, C. Chemical assembly of antibody-drug conjugates Next Generation Antibody Drug Conjugates (ADCs) and Immunotoxins. 1-28. 2017
report
- Calamini, B., Silva, M. C., Madoux, F., Hutt, D. M., Khanna, S., Chalfant, M. A., Allais, C., Ouizem, S., Saldanha, S. A., Ferguson, J., Mercer, B. A., Michael, C., et al. ML346: A novel modulator of proteostasis for protein conformational diseases 2010
- Minond, D., Saldanha, S. A., Spicer, T., Qin, L., Mercer, B. A., Roush, W. R., Hodder, P. HTS assay for discovery of novel metallo-beta-lactamase (MBL) inhibitors Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:21961119
- Busby, S., Nuhant, P., Cameron, M., Mercer, B. A., Hodder, P., Roush, W. R., Griffin, P. R. Discovery of inverse agonists for the liver receptor homologue-1 (LRH1; NR5A2) 2010
- Kumar, N., Nuhant, P., Solt, L. A., Conkright, J. J., Wang, Y., Istrate, M. A., Busby, S. A., Ruben, D. G. O., Burris, T. P., Cameron, M., Mercer, B. A., Hodder, P., et al. Identification of a novel selective inverse agonist probe and analogs for the Retinoic acid receptor-related Orphan Receptor Alpha (RORalpha) 2010
- Simanski, S., Madoux, F., Rahaim, R. J., Chase, P., Schurer, S., Cameron, M., Mercer, B. A., Hodder, P., Roush, W. R., Ayad, N. G. Identification of small molecule inhibitors of Wee1 degradation and mitotic entry 2010
- Kota, S., Madoux, F., Chase, P., Takahashi, V., Liu, Q., Mercer, B. A., Cameron, M., Strosberg, A. D., Roush, W., Hodder, P. ML322, a small molecule inhibitor of dimerization of the core protein of hepatitis C virus (HCV) 2010
- Cameron, M., Kamenecka, T., Madoux, F., Chase, P., Roush, W., Hodder, P., Griffin, P. R. ML368 identification of imidazopyridines as selective inhibitors of the cytochrome P450 enzyme CYP3A4 2010
- Spicer, T., Minond, D., Enogieru, I., Saldanha, S. A., Allais, C., Liu, Q., Mercer, B. A., Roush, W. R., Hodder, P. ML302, a novel beta-lactamase (BLA) inhibitor Probe Reports from the NIH Molecular Libraries Program. 2010 PMID:23762954
thesis
- A synthetic approach to dendrobine 1977

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