recent publications
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academic article
- Schnute, M. E., Wennerstal, M., Alley, J., Bengtsson, M., Blinn, J. R., Bolten, C. W., Braden, T., Bonn, T., Carlsson, B., Caspers, N., Chen, M., Choi, C., et al. Discovery of 3-cyano-N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo 2,3-b pyridin-5-yObenzamide: a potent, selective, and orally bioavailable retinoic acid receptor related orphan receptor C2 inverse agonist Journal of Medicinal Chemistry 2018 61:10415-10439 DOI:10.1021/acs.jmedchern.8b00392 PMID:30130103
- Vazquez, M. L., Kaila, N., Strohbach, J. W., Trzupek, J. D., Brown, M. F., Flanagan, M. E., Mitton-Fry, M. J., Johnson, T. A., TenBrink, R. E., Arnold, E. P., Basak, A., Heasley, S. E., et al. Identification of N-{cis-3-(methyl(7H-pyrrolo 2,3-d pyrimidin-4-yl)aminolcyclobutyl}propan e-1-sulfonamide (PF-04965842): a selective JAK1 clinical candidate for the treatment of autoimmune diseases Journal of Medicinal Chemistry 2018 61:1130-1152 DOI:10.1021/acs.jmedchem.7b01598 PMID:29298069
- Lee, K. L., Ambler, C. M., Anderson, D. R., Boscoe, B. P., Bree, A. G., Brodfuehrer, J. I., Chang, J. S., Choi, C., Chung, S., Curran, K. J., Day, J. E., Dehnhardt, C. M., et al. Discovery of clinical candidate 1-{ (2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl methoxy}-7-methoxyi soquinoline-6-carboxamide (PF-06650833), a potent, selective inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4), by fragment -based drug design Journal of Medicinal Chemistry 2017 60:5521-5542 DOI:10.1021/acs.jmedchem.7b00231 PMID:28498658
- Gerstenberger, B. S., Trzupek, J. D., Tallant, C., Fedorov, O., Filippakopoulos, P., Brennan, P. E., Fedele, V., Martin, S., Picaud, S., Rogers, C., Parikh, M., Taylor, A., et al. Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit Journal of Medicinal Chemistry 2016 59:4800-4811 DOI:10.1021/acs.jmedchem.6b00012 PMID:27115555 PMCID:PMC5034155
- Fedorov, O., Castex, J., Tallant, C., Owen, D. R., Martin, S., Aldeghi, M., Monteiro, O., Filippakopoulos, P., Picaud, S., Trzupek, J. D., Gerstenberger, B. S., Bountra, C., et al. Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance Science Advances 2015 1 DOI:10.1126/sciadv.1500723 PMID:26702435 PMCID:PMC4681344
- Fish, P. V., Filippakopoulos, P., Bish, G., Brennan, P. E., Bunnage, M. E., Cook, A. S., Federov, O., Gerstenberger, B. S., Jones, H., Knapp, S., Marsden, B., Nocka, K., et al. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit Journal of Medicinal Chemistry 2012 55:9831-9837 DOI:10.1021/jm3010515 PMID:23095041 PMCID:PMC3506127
- Trzupek, J. D., Li, C., Chan, C., Crowley, B. M., Heimann, A. C., Danishefsky, S. J. Lessons from the total synthesis of (+/-)-phalarine: insights into the mechanism of the Pictet-Spengler reaction Pure and Applied Chemistry 2010 82:1735-1748 DOI:10.1351/pac-con-09-11-14 PMID:20711493 PMCID:PMC2920150
- Trzupek, J. D., Lee, D., Crowley, B. M., Marathias, V. M., Danishefsky, S. J. Total synthesis of enantiopure phalarine via a stereospecific Pictet-Spengler reaction: traceless transfer of chirality from L-tryptophan Journal of the American Chemical Society 2010 132:8506-8512 DOI:10.1021/ja1030968 PMID:20509657 PMCID:PMC2895623
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Shimamura, H., Breazzano, S. P., Garfunkle, J., Kimball, F. S., Trzupek, J. D., Boger, D. L.
Total synthesis of complestatin: development of a Pd(0)-mediated indole annulation for macrocyclization
Journal of the American Chemical Society
2010
132:7776-7783
DOI:10.1021/ja102304p
PMID:20469945
PMCID:PMC2892899
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Garfunkle, J., Kimball, F. S., Trzupek, J. D., Takizawa, S., Shimamura, H., Tomishima, M., Boger, D. L.
Total synthesis of chloropeptin II (complestatin) and chloropeptin I
Journal of the American Chemical Society
2009
131:16036-16038
DOI:10.1021/ja907193b
PMID:19839632
PMCID:PMC2783344
- Kan, C., Trzupek, J. D., Wu, B., Chen, G., Tan, Z., Yuan, Y., Danishefsky, S. J. Toward homogeneous erythropoietin: chemical synthesis of the Ala1-Gly28 glycopeptide domain by "alanine" ligation Journal of the American Chemical Society 2009 131:5438-5443 DOI:10.1021/ja808707w PMID:19334679 PMCID:PMC2765573
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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
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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
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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
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Trzupek, J. D., Gottesfeld, J. M., Boger, D. L.
Alkylation of duplex DNA in nucleosome core particles by duocarmycin SA and yatakemycin
Nature Chemical Biology
2006
2:79-82
DOI:10.1038/nchembio761
PMID:16415862
- Toth, J. L., Trzupek, J. D., Flores, L. V., Kiakos, K., Hartley, J. A., Pennington, W. T., Lee, M. A novel achiral seco-amino-cyclopropylindoline (CI) analog of CC-1065 and the duocarmycins: design, synthesis and biological studies Medicinal Chemistry (Shariqah (United Arab Emirates)) 2005 1:13-9 PMID:16789881
- Trzupek, J. D., Sheppard, T. L. Photochemical generation of ribose abasic sites in RNA oligonucleotides Organic Letters 2005 7:1493-1496 DOI:10.1021/ol050120h PMID:15816735
- Kupchinsky, S., Centioni, S., Howard, T., Trzupek, J., Roller, S., Carnahan, V., Townes, H., Purnell, B., Price, C., Handl, H., Summerville, K., Johnson, K., et al. A novel class of achiral seco-analogs of CC-1065 and the duocarmycins: design, synthesis, DNA binding, and anticancer properties Bioorganic & Medicinal Chemistry 2004 12:6221-6236 DOI:10.1016/j.bmc.2004.08.051 PMID:15519165
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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