Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.

Smith, Aaron; Ni, Zhi-Jie; Poon, Daniel; Huang, Zilin; Chen, Zheng; Zhang, Qiong; Tandeske, Laura; Merritt, Hanne; Shoemaker, Kevin; Chan, John; Kaufman, Susan; Huh, Kay; Murray, Jeremy; Appleton, Brent A; Cowan-Jacob, Sandra W; Scheufler, Clemens; Kanazawa, Takanori; Jansen, Johanna M; Stuart, Darrin; Shafer, Cynthia M

Smith, Aaron; Ni, Zhi-Jie; Poon, Daniel; Huang, Zilin; Chen, Zheng; Zhang, Qiong; Tandeske, Laura; Merritt, Hanne; Shoemaker, Kevin; Chan, John; Kaufman, Susan; Huh, Kay; Murray, Jeremy; Appleton, Brent A; Cowan-Jacob, Sandra W; Scheufler, Clemens; Kanazawa, Takanori; Jansen, Johanna M; Stuart, Darrin; Shafer, Cynthia M.

Afiliação

Smith A; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Ni ZJ; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Poon D; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Huang Z; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Chen Z; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Zhang Q; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Tandeske L; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Merritt H; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Shoemaker K; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Chan J; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Kaufman S; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Huh K; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Murray J; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Appleton BA; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Cowan-Jacob SW; Novartis Institutes of Biomedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
Scheufler C; Novartis Institutes of Biomedical Research, Novartis Campus, CH-4056 Basel, Switzerland.
Kanazawa T; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Jansen JM; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Stuart D; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States.
Shafer CM; Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 5300 Chiron Way, Emeryville, CA 94608, United States. Electronic address: cynthia.shafer@novartis.com.

Bioorg Med Chem Lett ; 27(23): 5221-5224, 2017 12 01.

Article em En | MEDLINE | ID: mdl-29107542

ABSTRACT

ABSTRACT

A series of imidazo[1,2-a]pyridin-6-yl-benzamide analogs was designed as inhibitors of B-RAFV600E. Medicinal chemistry techniques were employed to explore the SAR for this series and improve selectivity versus P38 and VEGFR2.

Assuntos

Benzamidas/farmacologia; Compostos Heterocíclicos com 2 Anéis/farmacologia; Inibidores de Proteínas Quinases/farmacologia; Proteínas Proto-Oncogênicas B-raf/antagonistas & inibidores; Benzamidas/síntese química; Benzamidas/química; Relação Dose-Resposta a Droga; Compostos Heterocíclicos com 2 Anéis/síntese química; Compostos Heterocíclicos com 2 Anéis/química; Humanos; Modelos Moleculares; Estrutura Molecular; Inibidores de Proteínas Quinases/síntese química; Inibidores de Proteínas Quinases/química; Proteínas Proto-Oncogênicas B-raf/metabolismo; Relação Estrutura-Atividade

Palavras-chave

Kinase; MAPK; RAF

Texto completo

Adicionar na Minha BVS

Imprimir

XML

PubMed Links

Buscar no Google

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Benzamidas / Proteínas Proto-Oncogênicas B-raf / Inibidores de Proteínas Quinases / Compostos Heterocíclicos com 2 Anéis Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Estados Unidos

Texto completo

Adicionar na Minha BVS

Imprimir

XML

PubMed Links

Buscar no Google