Rational design and synthesis of 2,4-dichloro-6-methyl pyrimidine derivatives as potential selective EGFR<sup>T790M/L858R</sup> inhibitors for the treatment of non-small cell lung cancer.

Duan, Lei; Chu, Cilong; Huang, Xiaoling; Yao, Huizhi; Wen, Jie; Chen, Rui; Wang, Caolin; Tu, Yuanbiao; Lv, Qiaoli; Pan, Qingshan; Xu, Shan

Rational design and synthesis of 2,4-dichloro-6-methyl pyrimidine derivatives as potential selective EGFR^T790M/L858R inhibitors for the treatment of non-small cell lung cancer.

Duan, Lei; Chu, Cilong; Huang, Xiaoling; Yao, Huizhi; Wen, Jie; Chen, Rui; Wang, Caolin; Tu, Yuanbiao; Lv, Qiaoli; Pan, Qingshan; Xu, Shan.

Afiliação

Duan L; Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, Jiangxi Science & Technology Normal University, Nanchang, Jiangxi, China.
Chu C; Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, Jiangxi Science & Technology Normal University, Nanchang, Jiangxi, China.
Huang X; Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, Jiangxi Science & Technology Normal University, Nanchang, Jiangxi, China.
Yao H; Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, Jiangxi Science & Technology Normal University, Nanchang, Jiangxi, China.
Wen J; Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, Jiangxi Science & Technology Normal University, Nanchang, Jiangxi, China.
Chen R; Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, Jiangxi Science & Technology Normal University, Nanchang, Jiangxi, China.
Wang C; School of Pharmacy, East China University of Science & Technology, Shanghai, China.
Tu Y; Cancer Research Center, Jangxi University of Traditional Chinese Medicine, Nanchang, China.
Lv Q; Jiangxi Key Laboratory of Translational Cancer Research, Jiangxi Cancer Hospital, Nanchang, Jiangxi, People's Republic of China.
Pan Q; Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, Jiangxi Science & Technology Normal University, Nanchang, Jiangxi, China.
Xu S; Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, Jiangxi Science & Technology Normal University, Nanchang, Jiangxi, China.

Arch Pharm (Weinheim) ; 357(5): e2300736, 2024 May.

Article em En | MEDLINE | ID: mdl-38381049

Assuntos

Antineoplásicos; Apoptose; Carcinoma Pulmonar de Células não Pequenas; Proliferação de Células; Relação Dose-Resposta a Droga; Desenho de Fármacos; Receptores ErbB; Neoplasias Pulmonares; Inibidores de Proteínas Quinases; Pirimidinas; Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico; Carcinoma Pulmonar de Células não Pequenas/patologia; Humanos; Receptores ErbB/antagonistas & inibidores; Receptores ErbB/metabolismo; Neoplasias Pulmonares/tratamento farmacológico; Neoplasias Pulmonares/patologia; Pirimidinas/farmacologia; Pirimidinas/síntese química; Pirimidinas/química; Animais; Antineoplásicos/farmacologia; Antineoplásicos/síntese química; Antineoplásicos/química; Proliferação de Células/efeitos dos fármacos; Relação Estrutura-Atividade; Apoptose/efeitos dos fármacos; Camundongos; Inibidores de Proteínas Quinases/farmacologia; Inibidores de Proteínas Quinases/síntese química; Inibidores de Proteínas Quinases/química; Linhagem Celular Tumoral; Movimento Celular/efeitos dos fármacos; Estrutura Molecular; Camundongos Nus; Ensaios Antitumorais Modelo de Xenoenxerto; Camundongos Endogâmicos BALB C

Palavras-chave

EGFR; NSCLC; T790M/L858R mutation; docking; patientderived xenograft

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Desenho de Fármacos / Apoptose / Carcinoma Pulmonar de Células não Pequenas / Inibidores de Proteínas Quinases / Proliferação de Células / Relação Dose-Resposta a Droga / Receptores ErbB / Neoplasias Pulmonares / Antineoplásicos Limite: Animals / Humans Idioma: En Ano de publicação: 2024 Tipo de documento: Article

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