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Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2h)-one (PF-06821497)

Pei-Pei Kung,Patrick Bingham,Alexei Brooun,Michael Collins,Ya-Li Deng,Dac Dinh,Connie Fan,Ketan S. Gajiwala, Rita Grantner,Hovhannes J. Gukasyan,Wenyue Hu,Buwen Huang,Robert Kania,Susan E. Kephart,Cody Krivacic,Robert A. Kumpf,Penney Khamphavong,Manfred Kraus,Wei Liu,Karen A. Maegley,Lisa Nguyen,Shijian Ren,Dan Richter, Robert A. Rollins,Neal Sach,Shikhar Sharma,John Sherrill,Jillian Spangler,Albert E. Stewart,Scott Sutton,Sean Uryu,Dominique Verhelle,Hui Wang,Shuiwang Wang,Martin Wythes,Shuibo Xin,Shinji Yamazaki,Huichun Zhu,JinJiang Zhu,Luke Zehnder,Martin Edwards

Journal of medicinal chemistry（2017）

Cited 85|Views36
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