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Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors.
Xiang, Hao-Yue; Wang, Xiang; Chen, Yan-Hong; Zhang, Xi; Tan, Cun; Wang, Yi; Su, Yi; Gao, Zhi-Wei; Chen, Xiao-Yan; Xiong, Bing; Gao, Zhao-Bing; Chen, Yi; Ding, Jian; Meng, Ling-Hua; Yang, Chun-Hao.
Afiliação
  • Xiang HY; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China; College of Chemistry and Chemical Engineering, Central South University, Changsha, 410083, PR China.
  • Wang X; Division of Anti-tumor Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Chen YH; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Zhang X; Division of Anti-tumor Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Tan C; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Wang Y; Division of Anti-tumor Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Su Y; Division of Anti-tumor Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Gao ZW; Center for Drug Metabolism Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Chen XY; Center for Drug Metabolism Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Xiong B; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Gao ZB; Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Chen Y; Division of Anti-tumor Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China.
  • Ding J; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China; Division of Anti-tumor Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China; Shanghai HaiHe Pharmaceutical Co.
  • Meng LH; Division of Anti-tumor Pharmacology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China. Electronic address: lhmeng@simm.ac.cn.
  • Yang CH; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China. Electronic address: chyang@simm.ac.cn.
Eur J Med Chem ; 209: 112913, 2021 Jan 01.
Article em En | MEDLINE | ID: mdl-33109399

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperazinas / Pirróis / Morfolinas / Fosfatidilinositol 3-Quinases / Inibidores da Angiogênese / Inibidores de Fosfoinositídeo-3 Quinase / Antineoplásicos Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Animals / Female / Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2021 Tipo de documento: Article País de publicação: França

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperazinas / Pirróis / Morfolinas / Fosfatidilinositol 3-Quinases / Inibidores da Angiogênese / Inibidores de Fosfoinositídeo-3 Quinase / Antineoplásicos Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Animals / Female / Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2021 Tipo de documento: Article País de publicação: França