Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1

[Image: see text] High throughput screening and subsequent hit validation identified 4-isopropyl-3-(2-((1-phenylethyl)amino)pyrimidin-4-yl)oxazolidin-2-one as a potent inhibitor of IDH1(R132H). Synthesis of the four separate stereoisomers identified the (S,S)-diastereomer (IDH125, 1f) as the most po...

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Detaylı Bibliyografya
Yayımlandı:ACS Med Chem Lett
Asıl Yazarlar: Levell, Julian R., Caferro, Thomas, Chenail, Gregg, Dix, Ina, Dooley, Julia, Firestone, Brant, Fortin, Pascal D., Giraldes, John, Gould, Ty, Growney, Joseph D., Jones, Michael D., Kulathila, Raviraj, Lin, Fallon, Liu, Gang, Mueller, Arne, van der Plas, Simon, Slocum, Kelly, Smith, Troy, Terranova, Remi, Touré, B. Barry, Tyagi, Viraj, Wagner, Trixie, Xie, Xiaoling, Xu, Ming, Yang, Fan S., Zhou, Liping X., Pagliarini, Raymond, Cho, Young Shin
Materyal Türü: Artigo
Dil:Inglês
Baskı/Yayın Bilgisi: American Chemical Society 2016
Online Erişim:https://ncbi.nlm.nih.gov/pmc/articles/PMC5304300/
https://ncbi.nlm.nih.gov/pubmed/28197303
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00334
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