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Page 1
C-H methylation of heteroarenes inspired by radical SAM methyl transferase.
Gui J, Zhou Q, Pan CM, Yabe Y, Burns AC, Collins MR, Ornelas MA, Ishihara Y, Baran PS. Gui J, et al. Among authors: ornelas ma. J Am Chem Soc. 2014 Apr 2;136(13):4853-6. doi: 10.1021/ja5007838. Epub 2014 Mar 21. J Am Chem Soc. 2014. PMID: 24611732 Free PMC article.
A simple litmus test for aldehyde oxidase metabolism of heteroarenes.
O'Hara F, Burns AC, Collins MR, Dalvie D, Ornelas MA, Vaz AD, Fujiwara Y, Baran PS. O'Hara F, et al. Among authors: ornelas ma. J Med Chem. 2014 Feb 27;57(4):1616-20. doi: 10.1021/jm4017976. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24472070 Free PMC article.
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
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: ornelas ma. 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
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: ornelas ma. 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
21 results