Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H<sub>2</sub>S) donors as potent EGFR inhibitors against L858R resistance mutation.

Zheng, You-Guang; Zhang, Wu-Qi; Meng, Long; Wu, Xiao-Qing; Zhang, Ling; An, Lin; Li, Cheng-Lin; Gao, Cai-Yun; Xu, Liang; Liu, Yi

Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H₂S) donors as potent EGFR inhibitors against L858R resistance mutation.

Zheng, You-Guang; Zhang, Wu-Qi; Meng, Long; Wu, Xiao-Qing; Zhang, Ling; An, Lin; Li, Cheng-Lin; Gao, Cai-Yun; Xu, Liang; Liu, Yi.

Afiliação

Zheng YG; College of Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China; Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China. Electronic address: zhengyouguang@xzhmu.edu.cn.
Zhang WQ; College of Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China; Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China.
Meng L; College of Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China; Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China.
Wu XQ; Department of Molecular Biosciences, University of Kansas, Lawrence, KS, USA.
Zhang L; College of Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China; Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China.
An L; College of Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China; Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China.
Li CL; College of Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China; Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China.
Gao CY; College of Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China; Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China.
Xu L; Department of Molecular Biosciences, University of Kansas, Lawrence, KS, USA; Department of Radiation Oncology, The University of Kansas Medical Center, Kansas City, KS, USA.
Liu Y; College of Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China; Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical University, Xuzhou, 221004, PR China.

Eur J Med Chem ; 202: 112522, 2020 Sep 15.

Article em En | MEDLINE | ID: mdl-32619886

Assuntos

Compostos de Anilina/farmacologia; Antineoplásicos/farmacologia; Desenho de Fármacos; Sulfeto de Hidrogênio/farmacologia; Inibidores de Proteínas Quinases/farmacologia; Quinazolinas/farmacologia; Compostos de Anilina/síntese química; Compostos de Anilina/química; Antineoplásicos/síntese química; Antineoplásicos/química; Pontos de Checagem do Ciclo Celular/efeitos dos fármacos; Linhagem Celular; Proliferação de Células/efeitos dos fármacos; Sobrevivência Celular/efeitos dos fármacos; Relação Dose-Resposta a Droga; Ensaios de Seleção de Medicamentos Antitumorais; Receptores ErbB/antagonistas & inibidores; Receptores ErbB/genética; Receptores ErbB/metabolismo; Humanos; Sulfeto de Hidrogênio/química; Estrutura Molecular; Mutação; Inibidores de Proteínas Quinases/síntese química; Inibidores de Proteínas Quinases/química; Quinazolinas/síntese química; Quinazolinas/química; Relação Estrutura-Atividade

Palavras-chave

Conjugate; EGFR; H3255 (L858R); Hydrogen sulfide

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Quinazolinas / Desenho de Fármacos / Inibidores de Proteínas Quinases / Sulfeto de Hidrogênio / Compostos de Anilina / Antineoplásicos Idioma: En Ano de publicação: 2020 Tipo de documento: Article

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