Design, synthesis, structure-activity relationships study and X-ray crystallography of 3-substituted-indolin-2-one-5-carboxamide derivatives as PAK4 inhibitors.

Guo, Jing; Zhao, Fan; Yin, Wenbo; Zhu, Mingyue; Hao, Chenzhou; Pang, Yu; Wu, Tianxiao; Wang, Jian; Zhao, Dongmei; Li, Haitao; Cheng, Maosheng

Guo, Jing; Zhao, Fan; Yin, Wenbo; Zhu, Mingyue; Hao, Chenzhou; Pang, Yu; Wu, Tianxiao; Wang, Jian; Zhao, Dongmei; Li, Haitao; Cheng, Maosheng.

Afiliação

Guo J; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Zhao F; Tsinghua-Peking Joint Center for Life Sciences, Beijing Advanced Innovation Center for Structural Biology, Department of Basic Medical Sciences, School of Medicine, Tsinghua University, Beijing, 100084, China.
Yin W; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Zhu M; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Hao C; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Pang Y; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Wu T; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Wang J; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Zhao D; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China. Electronic address: dongmeiz-67@163.com.
Li H; Tsinghua-Peking Joint Center for Life Sciences, Beijing Advanced Innovation Center for Structural Biology, Department of Basic Medical Sciences, School of Medicine, Tsinghua University, Beijing, 100084, China. Electronic address: lht@tsinghua.edu.cn.
Cheng M; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China. Electronic address: mscheng@263.net.

Eur J Med Chem ; 155: 197-209, 2018 Jul 15.

Article em En | MEDLINE | ID: mdl-29886323

Assuntos

Antineoplásicos/farmacologia; Desenho de Fármacos; Inibidores Enzimáticos/farmacologia; Indóis/farmacologia; Quinases Ativadas por p21/antagonistas & inibidores; Antineoplásicos/síntese química; Antineoplásicos/química; Linhagem Celular Tumoral; Proliferação de Células/efeitos dos fármacos; Cristalografia por Raios X; Sistema Enzimático do Citocromo P-450/metabolismo; Relação Dose-Resposta a Droga; Ensaios de Seleção de Medicamentos Antitumorais; Inibidores Enzimáticos/síntese química; Inibidores Enzimáticos/química; Humanos; Indóis/síntese química; Indóis/química; Modelos Moleculares; Estrutura Molecular; Relação Estrutura-Atividade; Quinases Ativadas por p21/isolamento & purificação; Quinases Ativadas por p21/metabolismo

Palavras-chave

Indolin-2-one; X-ray crystallography; p21-activated kinase 4

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Inibidores Enzimáticos / Quinases Ativadas por p21 / Indóis / Antineoplásicos Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2018 Tipo de documento: Article País de afiliação: China País de publicação: França

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