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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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: 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
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2018
Acesso em linha: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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