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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Veröffentlicht in:ACS Med Chem Lett
Hauptverfasser: 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
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2018
Online Zugang: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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