Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.

Aman, Waqar; Lee, Junghun; Kim, Minjung; Yang, Songyi; Jung, Hoyong; Hah, Jung-Mi

Aman, Waqar; Lee, Junghun; Kim, Minjung; Yang, Songyi; Jung, Hoyong; Hah, Jung-Mi.

Afiliação

Aman W; Department of Pharmacy, College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do 426-791, Republic of Korea.
Lee J; Department of Pharmacy, College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do 426-791, Republic of Korea.
Kim M; Department of Pharmacy, College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do 426-791, Republic of Korea.
Yang S; Department of Pharmacy, College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do 426-791, Republic of Korea.
Jung H; Department of Pharmacy, College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do 426-791, Republic of Korea.
Hah JM; Department of Pharmacy, College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do 426-791, Republic of Korea. Electronic address: jhah@hanyang.ac.kr.

Bioorg Med Chem Lett ; 26(4): 1188-92, 2016 Feb 15.

Article em En | MEDLINE | ID: mdl-26810260

Assuntos

Amidas/química; Desenho de Fármacos; Indazóis/química; Inibidores de Proteínas Quinases/síntese química; Proteínas Proto-Oncogênicas c-raf/antagonistas & inibidores; Amidas/síntese química; Amidas/farmacologia; Sítios de Ligação; Linhagem Celular Tumoral; Proliferação de Células/efeitos dos fármacos; Humanos; Simulação de Acoplamento Molecular; Inibidores de Proteínas Quinases/química; Inibidores de Proteínas Quinases/toxicidade; Estrutura Terciária de Proteína; Proteínas Proto-Oncogênicas c-raf/metabolismo

Palavras-chave

BRAF V600E; CRAF; Melanoma; Selectivity

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Proteínas Proto-Oncogênicas c-raf / Inibidores de Proteínas Quinases / Amidas / Indazóis Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article

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