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Page 1
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).
Kung PP, Bingham P, Brooun A, Collins M, Deng YL, Dinh D, Fan C, Gajiwala KS, Grantner R, Gukasyan HJ, Hu W, Huang B, Kania R, Kephart SE, Krivacic C, Kumpf RA, Khamphavong P, Kraus M, Liu W, Maegley KA, Nguyen L, Ren S, Richter D, Rollins RA, Sach N, Sharma S, Sherrill J, Spangler J, Stewart AE, Sutton S, Uryu S, Verhelle D, Wang H, Wang S, Wythes M, Xin S, Yamazaki S, Zhu H, Zhu J, Zehnder L, Edwards M. Kung PP, et al. Among authors: kephart se. J Med Chem. 2018 Feb 8;61(3):650-665. doi: 10.1021/acs.jmedchem.7b01375. Epub 2017 Dec 27. J Med Chem. 2018. PMID: 29211475
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. 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. 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
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).
Cheng H, Orr STM, Bailey S, Brooun A, Chen P, Deal JG, Deng YL, Edwards MP, Gallego GM, Grodsky N, Huang B, Jalaie M, Kaiser S, Kania RS, Kephart SE, Lafontaine J, Ornelas MA, Pairish M, Planken S, Shen H, Sutton S, Zehnder L, Almaden CD, Bagrodia S, Falk MD, Gukasyan HJ, Ho C, Kang X, Kosa RE, Liu L, Spilker ME, Timofeevski S, Visswanathan R, Wang Z, Meng F, Ren S, Shao L, Xu F, Kath JC. Cheng H, et al. Among authors: kephart se. J Med Chem. 2021 Jan 14;64(1):644-661. doi: 10.1021/acs.jmedchem.0c01652. Epub 2020 Dec 24. J Med Chem. 2021. PMID: 33356246
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. J Med Chem. 2012 May 24;55(10):4728-39. doi: 10.1021/jm300204j. Epub 2012 May 14. J Med Chem. 2012. PMID: 22554206
Correction to 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. J Med Chem. 2016 Dec 22;59(24):11196. doi: 10.1021/acs.jmedchem.6b01747. Epub 2016 Dec 12. J Med Chem. 2016. PMID: 27936698 No abstract available.
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
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. J Med Chem. 2011 Nov 10;54(21):7693-704. doi: 10.1021/jm201059s. Epub 2011 Oct 7. J Med Chem. 2011. PMID: 21936524
19 results