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Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.
J Med Chem ; 52(5): 1251-4, 2009 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-19260711
ABSTRACT
Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of the pyridine 3-position gave improved enzyme potency, while substitution of the pyridone 4-position led to improved aqueous solubility and kinase selectivity. Analogue 10 demonstrated complete tumor stasis in a Met-dependent GTL-16 human gastric carcinoma xenograft model following oral administration. Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclinical safety profiles, 10 has been advanced into phase I clinical trials.
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Texto completo: Disponível Coleções: Bases de dados internacionais Base de dados: MEDLINE Assunto principal: Piridonas / Di-Hidropiridinas / Proteínas Proto-Oncogênicas c-met / Aminopiridinas / Antineoplásicos Limite: Animais / Humanos Idioma: Inglês Revista: J Med Chem Assunto da revista: Química Ano de publicação: 2009 Tipo de documento: Artigo País de afiliação: Estados Unidos