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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).
Kung, Pei-Pei; Bingham, Patrick; Brooun, Alexei; Collins, Michael; Deng, Ya-Li; Dinh, Dac; Fan, Connie; Gajiwala, Ketan S; Grantner, Rita; Gukasyan, Hovhannes J; Hu, Wenyue; Huang, Buwen; Kania, Robert; Kephart, Susan E; Krivacic, Cody; Kumpf, Robert A; Khamphavong, Penney; Kraus, Manfred; Liu, Wei; Maegley, Karen A; Nguyen, Lisa; Ren, Shijian; Richter, Dan; Rollins, Robert A; Sach, Neal; Sharma, Shikhar; Sherrill, John; Spangler, Jillian; Stewart, Albert E; Sutton, Scott; Uryu, Sean; Verhelle, Dominique; Wang, Hui; Wang, Shuiwang; Wythes, Martin; Xin, Shuibo; Yamazaki, Shinji; Zhu, Huichun; Zhu, JinJiang; Zehnder, Luke; Edwards, Martin.
Afiliación
  • Ren S; WuXi AppTec , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
  • Rollins RA; Pfizer Global Research and Development , 401 N. Middletown Road, Pearl River, New York 10965, United States.
  • Wang S; WuXi AppTec , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
  • Xin S; WuXi AppTec , 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
J Med Chem ; 61(3): 650-665, 2018 02 08.
Article en En | MEDLINE | ID: mdl-29211475
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Diseño de Fármacos / Proteína Potenciadora del Homólogo Zeste 2 / Isoquinolinas Tipo de estudio: Diagnostic_studies Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article
Texto completo
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Diseño de Fármacos / Proteína Potenciadora del Homólogo Zeste 2 / Isoquinolinas Tipo de estudio: Diagnostic_studies Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article