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Page 1
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.
Levell JR, Caferro T, Chenail G, Dix I, Dooley J, Firestone B, Fortin PD, Giraldes J, Gould T, Growney JD, Jones MD, Kulathila R, Lin F, Liu G, Mueller A, van der Plas S, Slocum K, Smith T, Terranova R, Touré BB, Tyagi V, Wagner T, Xie X, Xu M, Yang FS, Zhou LX, Pagliarini R, Cho YS. Levell JR, et al. Among authors: chenail g. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156. doi: 10.1021/acsmedchemlett.6b00334. eCollection 2017 Feb 9. ACS Med Chem Lett. 2016. PMID: 28197303 Free PMC article.
Allosteric Mutant IDH1 Inhibitors Reveal Mechanisms for IDH1 Mutant and Isoform Selectivity.
Xie X, Baird D, Bowen K, Capka V, Chen J, Chenail G, Cho Y, Dooley J, Farsidjani A, Fortin P, Kohls D, Kulathila R, Lin F, McKay D, Rodrigues L, Sage D, Touré BB, van der Plas S, Wright K, Xu M, Yin H, Levell J, Pagliarini RA. Xie X, et al. Among authors: chenail g. Structure. 2017 Mar 7;25(3):506-513. doi: 10.1016/j.str.2016.12.017. Epub 2017 Jan 26. Structure. 2017. PMID: 28132785 Free article.
Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor.
Cho YS, Levell JR, Liu G, Caferro T, Sutton J, Shafer CM, Costales A, Manning JR, Zhao Q, Sendzik M, Shultz M, Chenail G, Dooley J, Villalba B, Farsidjani A, Chen J, Kulathila R, Xie X, Dodd S, Gould T, Liang G, Heimbach T, Slocum K, Firestone B, Pu M, Pagliarini R, Growney JD. Cho YS, et al. Among authors: chenail g. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121. doi: 10.1021/acsmedchemlett.7b00342. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057061 Free PMC article.
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors.
Zhao Q, Manning JR, Sutton J, Costales A, Sendzik M, Shafer CM, Levell JR, Liu G, Caferro T, Cho YS, Palermo M, Chenail G, Dooley J, Villalba B, Farsidjani A, Chen J, Dodd S, Gould T, Liang G, Slocum K, Pu M, Firestone B, Growney J, Heimbach T, Pagliarini R. Zhao Q, et al. Among authors: chenail g. ACS Med Chem Lett. 2018 Jun 11;9(7):746-751. doi: 10.1021/acsmedchemlett.8b00182. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034612 Free PMC article.
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Papillon JPN, Nakajima K, Adair CD, Hempel J, Jouk AO, Karki RG, Mathieu S, Möbitz H, Ntaganda R, Smith T, Visser M, Hill SE, Hurtado FK, Chenail G, Bhang HC, Bric A, Xiang K, Bushold G, Gilbert T, Vattay A, Dooley J, Costa EA, Park I, Li A, Farley D, Lounkine E, Yue QK, Xie X, Zhu X, Kulathila R, King D, Hu T, Vulic K, Cantwell J, Luu C, Jagani Z. Papillon JPN, et al. Among authors: chenail g. J Med Chem. 2018 Nov 21;61(22):10155-10172. doi: 10.1021/acs.jmedchem.8b01318. Epub 2018 Oct 31. J Med Chem. 2018. PMID: 30339381