recent publications

• academic article

  • Robertson, W. M., Kastrinsky, D. B., Hwang, I., Boger, D. L. Synthesis and evaluation of a series of C5'-substituted duocarmycin SA analogs Bioorganic & Medicinal Chemistry Letters  2010 20:2722-2725  DOI:10.1016/j.bmcl.2010.03.078  PMID:20381346  PMCID:PMC2867475
  • MacMillan, K. S., Lajiness, J. P., Cara, C. L., Romagnoli, R., Robertson, W. M., Hwang, I., Baraldi, P. G., Boger, D. L. Synthesis and evaluation of a thio analogue of duocarmycin SA Bioorganic & Medicinal Chemistry Letters  2009 19:6962-6965  DOI:10.1016/j.bmcl.2009.10.063  PMID:19879753  PMCID:PMC2784222
  • Gauss, C. M., Hamasaki, A., Parrish, J. P., MacMillan, K. S., Rayl, T. J., Hwang, I., Boger, D. L. Synthesis and preliminary evaluation of duocarmycin analogues incorporating the 1,2,11,11a-tetrahydrocyclopropa c naphtho 2,3-e indol-4-one (CNI) and 1,2,11,11a-tetrahydrocyclopropa c naphtho 1,2-e indol-4-one (iso-CNI) alkylation subunits Tetrahedron  2009 65:6591-6599  DOI:10.1016/j.tet.2009.02.065  PMID:20161204  PMCID:PMC2713043
  • Clark, R. C., Lee, S. Y., Hwang, I., Searcey, M., Boger, D. L. Evaluation of chlorofusin, its seven chromophore diastereomers, and key analogues Tetrahedron Letters  2009 50:3151-3153  DOI:10.1016/j.tetlet.2009.01.081  PMID:20161293  PMCID:PMC2697908
  • Shaginian, A., Whitby, L. R., Hong, S., Hwang, I., Farooqi, B., Searcey, M., Chen, J. C., Vogt, P. K., Boger, D. L. Design, synthesis, and evaluation of an α-helix mimetic library targeting protein-protein interactions Journal of the American Chemical Society  2009 131:5564-5572  DOI:10.1021/ja810025g  PMID:19334711  PMCID:PMC2765553
  • Ishikawa, H., Colby, D. A., Seto, S., Va, P., Tam, A., Kakei, H., Rayl, T. J., Hwang, I., Boger, D. L. Total synthesis of vinblastine, vincristine, related natural products, and key structural analogues Journal of the American Chemical Society  2009 131:4904-4916  DOI:10.1021/ja809842b  PMID:19292450  PMCID:PMC2727944
  • MacMillan, K. S., Nguyen, T., Hwang, I., Boger, D. L. Total synthesis and evaluation of iso-duocarmycin SA and iso-yatakemycin Journal of the American Chemical Society  2009 131:1187-1194  DOI:10.1021/ja808108q  PMID:19154178  PMCID:PMC2646182
  • DeMartino, J. K., Hwang, I., Connelly, S., Wilson, I. A., Boger, D. L. Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase Journal of Medicinal Chemistry  2008 51:5441-5448  DOI:10.1021/jm800555h  PMID:18686942  PMCID:PMC2559975
  • Garfunkle, J., Ezzili, C., Rayl, T. J., Hochstatter, D. G., Hwang, I., Boger, D. L. Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase Journal of Medicinal Chemistry  2008 51:4392-4403  DOI:10.1021/jm800136b  PMID:18630870  PMCID:PMC2556205
  • Kimball, F. S., Romero, F. A., Ezzili, C., Garfunkle, J., Rayl, T. J., Hochstatter, D. G., Hwang, I., Boger, D. L. Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase Journal of Medicinal Chemistry  2008 51:937-947  DOI:10.1021/jm701210y  PMID:18247553  PMCID:PMC2734917
  • Jin, W., Trzupek, J. D., Rayl, T. J., Broward, M. A., Vielhauer, G. A., Weir, S. J., Hwang, I., Boger, D. L. A unique class of duocarmycin and CC-1065 analogues subject to reductive activation Journal of the American Chemical Society  2007 129:15391-15397  DOI:10.1021/ja075398e  PMID:18020335  PMCID:PMC2519901
  • Tichenor, M. S., MacMillan, K. S., Stover, J. S., Wolkenberg, S. E., Pavani, M. G., Zanella, L., Zaid, A. N., Spalluto, G., Rayl, T. J., Hwang, I., Baraldi, P. G., Boger, D. L. Rational design, synthesis, and evaluation of key analogues of CC-1065 and the duocarmycins Journal of the American Chemical Society  2007 129:14092-14099  DOI:10.1021/ja073989z  PMID:17948994  PMCID:PMC2531197
  • Tichenor, M. S., MacMillan, K. S., Trzupek, J. D., Rayl, T. J., Hwang, I., Boger, D. L. Systematic exploration of the structural features of yatakemycin impacting DNA alkylation and biological activity Journal of the American Chemical Society  2007 129:10858-10869  DOI:10.1021/ja072777z  PMID:17691783  PMCID:PMC2519902
  • Hardouin, C., Kelso, M. J., Romero, F. A., Rayl, T. J., Leung, D., Hwang, I., Cravatt, B. F., Boger, D. L. Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase Journal of Medicinal Chemistry  2007 50:3359-3368  DOI:10.1021/jm061414r  PMID:17559203  PMCID:PMC2531194
  • Romero, F. A., Du, W., Hwang, I., Rayl, T. J., Kimball, F. S., Leung, D., Hoover, H. S., Apodaca, R. L., Breitenbucher, J. G., Cravatt, B. F., Boger, D. L. Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase Journal of Medicinal Chemistry  2007 50:1058-1068  DOI:10.1021/jm0611509  PMID:17279740  PMCID:PMC2531193
  • Tichenor, M. S., Trzupek, J. D., Kastrinsky, D. B., Shiga, F., Hwang, I., Boger, D. L. Asymmetric total synthesis of (+)- and ent-(-)-yatakemycin and duocarmycin SA: evaluation of yatakemycin key partial structures and its unnatural enantiomer Journal of the American Chemical Society  2006 128:15683-15696  DOI:10.1021/ja064228j  PMID:17147378  PMCID:PMC2515590
  • Romero, F. A., Hwang, I., Boger, D. L. Delineation of a fundamental alpha-ketoheterocycle substituent effect for use in the design of enzyme inhibitors Journal of the American Chemical Society  2006 128:14004-14005  DOI:10.1021/ja064522b  PMID:17061864  PMCID:PMC2501112
  • Schnermann, M. J., Romero, F. A., Hwang, I., Nakamaru-Ogiso, E., Yagi, T., Boger, D. L. Total synthesis of piericidin A1 and B1 and key analogues Journal of the American Chemical Society  2006 128:11799-11807  DOI:10.1021/ja0632862  PMID:16953619  PMCID:PMC2531196
  • DeMartino, J. K., Hwang, I., Xu, L., Wilson, I. A., Boger, D. L. Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase Journal of Medicinal Chemistry  2006 49:2998-3002  DOI:10.1021/jm0601147  PMID:16686541  PMCID:PMC2531195
  • Reader, J. S., Ordoukhanian, P. T., Kim, J. G., de Crecy-Lagard, V., Hwang, I., Farrand, S., Schimmel, P. Major biocontrol of plant tumors targets tRNA synthetase Science  2005 309:1533  DOI:10.1126/science.1116841  PMID:16141066
  • Hamasaki, A., Zimpleman, J. M., Hwang, I., Boger, D. L. Total synthesis of ningalin D Journal of the American Chemical Society  2005 127:10767-10770  DOI:10.1021/ja0526416  PMID:16045367  PMCID:PMC2480523
  • Capps, K. J., Humiston, J., Dominique, R., Hwang, I., Boger, D. L. Discovery of aicar tfase inhibitors that disrupt requisite enzyme dimerization Bioorganic & Medicinal Chemistry Letters  2005 15:2840-2844  DOI:10.1016/j.bcml.2005.03.094  PMID:15911265
  • Cheng, H., Chong, Y. H., Hwang, I., Tavassoli, A., Zhang, Y., Wilson, I. A., Benkovic, S. J., Boger, D. L. Design, synthesis, and biological evaluation of 10-methanesulfonyl-DDACTHF, 10-methanesulfonyl-5-DACTHF, and 10-methylthio-DDACTHF as potent inhibitors of GAR Tfase and the de novo purine biosynthetic pathway Bioorganic & Medicinal Chemistry  2005 13:3577-3585  DOI:10.1016/j.bmc.2004.12.004  PMID:15848770
  • Cheng, H., Hwang, I., Chong, Y. H., Tavassoli, A., Webb, M. E., Zhang, Y., Wilson, I. A., Benkovic, S. J., Boger, D. L. Synthesis and biological evaluation of N-{4- 5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoro acetyl)pentyl)benzoyl}-L-glutamic acid as a potential inhibitor of GAR Tfase and the de novo purine biosynthetic pathway Bioorganic & Medicinal Chemistry  2005 13:3593-3599  DOI:10.1016/j.bme.2004.11.049  PMID:15848772
  • Chong, Y., Hwang, I., Tavassoli, A., Zhang, Y., Wilson, I. A., Benkovic, S. J., Boger, D. L. Synthesis and biological evaluation of α- and γ-carboxamide derivatives of 10-CF3CO-DDACTHF Bioorganic & Medicinal Chemistry  2005 13:3587-3592  DOI:10.1016/j.bme.2004.11.050  PMID:15848771
  • Boger, D. L., Miyauchi, H., Du, W., Hardouin, C., Fecik, R. A., Cheng, H., Hwang, I., Hedrick, M. P., Leung, D., Acevedo, O., Guimaraes, C. R. W., Jorgensen, W. L., et al. Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics Journal of Medicinal Chemistry  2005 48:1849-1856  DOI:10.1021/jm049614v  PMID:15771430  PMCID:PMC2492884
  • Leung, D., Du, W., Hardouin, C., Cheng, H., Hwang, I., Cravatt, B. F., Boger, D. L. Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity Bioorganic & Medicinal Chemistry Letters  2005 15:1423-1428  DOI:10.1016/j.bmcl.2004.12.085  PMID:15713400
  • Du, W., Hardouin, C., Cheng, H., Hwang, I., Boger, D. L. Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase Bioorganic & Medicinal Chemistry Letters  2005 15:103-106  DOI:10.1016/j.bmcl.2004.10.025  PMID:15582420
  • Parrish, J. P., Trzupek, J. D., Hughes, T. V., Hwang, I., Boger, D. L. Synthesis and evaluation of N-aryl and N-alkenyl CBI derivatives Bioorganic & Medicinal Chemistry  2004 12:5845-5856  DOI:10.1016/j.bmc.2004.08.032  PMID:15498660
  • Rew, Y., Shin, D., Hwang, I., Boger, D. L. Total synthesis and examination of three key analogues of ramoplanin: a lipoglycodepsipeptide with potent antibiotic activity Journal of the American Chemical Society  2004 126:1041-1043  DOI:10.1021/ja039671y  PMID:14746470
  • Buck, S. B., Hardouin, C., Ichikawa, S., Soenen, D. R., Gauss, C. M., Hwang, I., Swingle, M. R., Bonness, K. M., Honkanen, R. E., Boger, D. L. Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition Journal of the American Chemical Society  2003 125:15694-15695  DOI:10.1021/ja038672n  PMID:14677930
  • Parrish, J. P., Kastrinsky, D. B., Hwang, I., Boger, D. L. Synthesis and evaluation of duocarmycin and CC-1065 analogues incorporating the 1,2,9,9a-tetrahydrocyclopropa c benz e -3-azaindol-4-one (CBA) alkylation subunit Journal of Organic Chemistry  2003 68:8984-8990  DOI:10.1021/jo035119f  PMID:14604371
  • Desharnais, J., Hwang, I., Zhang, Y., Tavassoli, A., Baboval, J., Benkovic, S. J., Wilson, I. A., Boger, D. L. Design, synthesis and biological evaluation of 10-CF3CO-DDACTHF analogues and derivatives as inhibitors of GAR Tfase and the de novo purine biosynthetic pathway Bioorganic & Medicinal Chemistry  2003 11:4511-4521  DOI:10.1016/s0968-0896(03)00458-9  PMID:13129587
  • Parrish, J. P., Kastrinsky, D. B., Stauffer, F., Hedrick, M. P., Hwang, I., Boger, D. L. Establishment of substituent effects in the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065 Bioorganic & Medicinal Chemistry  2003 11:3815-3838  DOI:10.1016/s0968-0896(03)00194-9  PMID:12901927
  • Soenen, D. R., Hwang, I., Hedrick, M. P., Boger, D. L. Multidrug resistance reversal activity of key ningalin analogues Bioorganic & Medicinal Chemistry Letters  2003 13:1777-1781  DOI:10.1016/s0960-894x(03)00294-4  PMID:12729663
  • McComas, C. C., Crowley, B. M., Hwang, I., Boger, D. L. Synthesis and evaluation of methyl ether derivatives of the vancomycin, teicoplanin, and ristocetin aglycon methyl esters Bioorganic & Medicinal Chemistry Letters  2003 13:2933-2936  DOI:10.1016/s0960-894x(03)00513-4  PMID:14611861
  • Hwang, I., Huang, J. F., Kishimoto, H., Brunmark, A., Peterson, P. A., Jackson, M. R., Surh, C. D., Cai, Z. L., Sprent, J. T cells can use either t cell receptor or cd28 receptors to absorb and internalize cell surface molecules derived from antigen-presenting cells Journal of Experimental Medicine  2000 191:1137-1148  DOI:10.1084/jem.191.7.1137  PMID:10748232