Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors

[Image: see text] Mutant isocitrate dehydrogenase 1 (IDH1) is an attractive therapeutic target for the treatment of various cancers such as AML, glioma, and glioblastoma. We have evaluated 3-pyrimidin-4-yl-oxazolidin-2-ones as mutant IDH1 inhibitors that bind to an allosteric, induced pocket of IDH1...

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Vydáno v:ACS Med Chem Lett
Hlavní autoři: Zhao, Qian, Manning, James R., Sutton, James, Costales, Abran, Sendzik, Martin, Shafer, Cynthia M., Levell, Julian R., Liu, Gang, Caferro, Thomas, Cho, Young Shin, Palermo, Mark, Chenail, Gregg, Dooley, Julia, Villalba, Brian, Farsidjani, Ali, Chen, Jinyun, Dodd, Stephanie, Gould, Ty, Liang, Guiqing, Slocum, Kelly, Pu, Minying, Firestone, Brant, Growney, Joseph, Heimbach, Tycho, Pagliarini, Raymond
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2018
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC6047033/
https://ncbi.nlm.nih.gov/pubmed/30034612
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00182
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