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Page 1
Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.
Guo C, McAlpine I, Zhang J, Knighton DD, Kephart S, Johnson MC, Li H, Bouzida D, Yang A, Dong L, Marakovits J, Tikhe J, Richardson P, Guo LC, Kania R, Edwards MP, Kraynov E, Christensen J, Piraino J, Lee J, Dagostino E, Del-Carmen C, Deng YL, Smeal T, Murray BW. Guo C, et al. Among authors: kephart s. J Med Chem. 2012 May 24;55(10):4728-39. doi: 10.1021/jm300204j. Epub 2012 May 14. J Med Chem. 2012. PMID: 22554206
Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
Guo C, Linton A, Kephart S, Ornelas M, Pairish M, Gonzalez J, Greasley S, Nagata A, Burke BJ, Edwards M, Hosea N, Kang P, Hu W, Engebretsen J, Briere D, Shi M, Gukasyan H, Richardson P, Dack K, Underwood T, Johnson P, Morell A, Felstead R, Kuruma H, Matsimoto H, Zoubeidi A, Gleave M, Los G, Fanjul AN. Guo C, et al. Among authors: kephart s. J Med Chem. 2011 Nov 10;54(21):7693-704. doi: 10.1021/jm201059s. Epub 2011 Oct 7. J Med Chem. 2011. PMID: 21936524
Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth.
Murray BW, Guo C, Piraino J, Westwick JK, Zhang C, Lamerdin J, Dagostino E, Knighton D, Loi CM, Zager M, Kraynov E, Popoff I, Christensen JG, Martinez R, Kephart SE, Marakovits J, Karlicek S, Bergqvist S, Smeal T. Murray BW, et al. Among authors: kephart se. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9446-51. doi: 10.1073/pnas.0911863107. Epub 2010 May 3. Proc Natl Acad Sci U S A. 2010. PMID: 20439741 Free PMC article.
Structural modifications of a 3-methoxy-2-aminopyridine compound to reduce potential for mutagenicity and time-dependent drug-drug interaction.
Palmer C, Pairish M, Kephart S, Bouzida D, Cui J, Deal J, Dong L, Gu D, Linton A, McAlpine I, Yamazaki S, Smith E, John-Baptiste A, Bagrodia S, Kania R, Guo C. Palmer C, et al. Among authors: kephart s. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7605-9. doi: 10.1016/j.bmcl.2012.10.011. Epub 2012 Oct 11. Bioorg Med Chem Lett. 2012. PMID: 23116892
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.
Cheng H, Nair SK, Murray BW, Almaden C, Bailey S, Baxi S, Behenna D, Cho-Schultz S, Dalvie D, Dinh DM, Edwards MP, Feng JL, Ferre RA, Gajiwala KS, Hemkens MD, Jackson-Fisher A, Jalaie M, Johnson TO, Kania RS, Kephart S, Lafontaine J, Lunney B, Liu KK, Liu Z, Matthews J, Nagata A, Niessen S, Ornelas MA, Orr ST, Pairish M, Planken S, Ren S, Richter D, Ryan K, Sach N, Shen H, Smeal T, Solowiej J, Sutton S, Tran K, Tseng E, Vernier W, Walls M, Wang S, Weinrich SL, Xin S, Xu H, Yin MJ, Zientek M, Zhou R, Kath JC. Cheng H, et al. Among authors: kephart s. J Med Chem. 2016 Mar 10;59(5):2005-24. doi: 10.1021/acs.jmedchem.5b01633. Epub 2016 Jan 28. J Med Chem. 2016. PMID: 26756222
Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M. Kung PP, et al. Among authors: kephart s. J Med Chem. 2016 Sep 22;59(18):8306-25. doi: 10.1021/acs.jmedchem.6b00515. Epub 2016 Sep 6. J Med Chem. 2016. PMID: 27512831
Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer.
Freeman-Cook KD, Hoffman RL, Behenna DC, Boras B, Carelli J, Diehl W, Ferre RA, He YA, Hui A, Huang B, Huser N, Jones R, Kephart SE, Lapek J, McTigue M, Miller N, Murray BW, Nagata A, Nguyen L, Niessen S, Ninkovic S, O'Doherty I, Ornelas MA, Solowiej J, Sutton SC, Tran K, Tseng E, Visswanathan R, Xu M, Zehnder L, Zhang Q, Zhang C, Dann S. Freeman-Cook KD, et al. Among authors: kephart se. J Med Chem. 2021 Jul 8;64(13):9056-9077. doi: 10.1021/acs.jmedchem.1c00159. Epub 2021 Jun 10. J Med Chem. 2021. PMID: 34110834
40 results