Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor

[Image: see text] Inhibition of mutant IDH1 is being evaluated clinically as a promising treatment option for various cancers with hotspot mutation at Arg(132). Having identified an allosteric, induced pocket of IDH1(R132H), we have explored 3-pyrimidin-4-yl-oxazolidin-2-ones as mutant IDH1 inhibito...

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Опубликовано в: :ACS Med Chem Lett
Главные авторы: Cho, Young Shin, Levell, Julian R., Liu, Gang, Caferro, Thomas, Sutton, James, Shafer, Cynthia M., Costales, Abran, Manning, James R., Zhao, Qian, Sendzik, Martin, Shultz, Michael, Chenail, Gregg, Dooley, Julia, Villalba, Brian, Farsidjani, Ali, Chen, Jinyun, Kulathila, Raviraj, Xie, Xiaoling, Dodd, Stephanie, Gould, Ty, Liang, Guiqing, Heimbach, Tycho, Slocum, Kelly, Firestone, Brant, Pu, Minying, Pagliarini, Raymond, Growney, Joseph D.
Формат: Artigo
Язык:Inglês
Опубликовано: American Chemical Society 2017
Online-ссылка:https://ncbi.nlm.nih.gov/pmc/articles/PMC5641959/
https://ncbi.nlm.nih.gov/pubmed/29057061
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.7b00342
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