Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC.

Pan, Tao; Dan, Yanrong; Guo, Dafeng; Jiang, Junhao; Ran, Dongzhi; Zhang, Lin; Tian, Binghua; Yuan, Jianyong; Yu, Yu; Gan, Zongjie

Pan, Tao; Dan, Yanrong; Guo, Dafeng; Jiang, Junhao; Ran, Dongzhi; Zhang, Lin; Tian, Binghua; Yuan, Jianyong; Yu, Yu; Gan, Zongjie.

Afiliação

Pan T; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Dan Y; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Guo D; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Jiang J; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China.
Ran D; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China.
Zhang L; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Tian B; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China.
Yuan J; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China.
Yu Y; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China. Electronic address: yuyu3519@163.com.
Gan Z; Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, PR China; Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China. Electronic address: gzj@cqmu.edu.cn.

Eur J Med Chem ; 224: 113672, 2021 Nov 15.

Article em En | MEDLINE | ID: mdl-34237620

Assuntos

Quinase do Linfoma Anaplásico/antagonistas & inibidores; Diaminas/química; Inibidores de Histona Desacetilases/química; Histona Desacetilases/química; Inibidores de Proteínas Quinases/química; Quinase do Linfoma Anaplásico/metabolismo; Antineoplásicos/química; Antineoplásicos/metabolismo; Antineoplásicos/farmacologia; Apoptose/efeitos dos fármacos; Sítios de Ligação; Pontos de Checagem do Ciclo Celular/efeitos dos fármacos; Linhagem Celular Tumoral; Movimento Celular/efeitos dos fármacos; Proliferação de Células/efeitos dos fármacos; Diaminas/metabolismo; Diaminas/farmacologia; Desenho de Fármacos; Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos; Ensaios de Seleção de Medicamentos Antitumorais; Inibidores de Histona Desacetilases/metabolismo; Inibidores de Histona Desacetilases/farmacologia; Histona Desacetilases/metabolismo; Humanos; Simulação de Dinâmica Molecular; Inibidores de Proteínas Quinases/metabolismo; Inibidores de Proteínas Quinases/farmacologia; Pirimidinas/química; Relação Estrutura-Atividade

Palavras-chave

2,4-Pyrimidinediamine; ALK/HDAC dual Inhibitors; NSCLC; Pharmacophore merged strategy

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Inibidores de Proteínas Quinases / Diaminas / Inibidores de Histona Desacetilases / Quinase do Linfoma Anaplásico / Histona Desacetilases Idioma: En Ano de publicação: 2021 Tipo de documento: Article

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