The discovery of benzanilides as c-Met receptor tyrosine kinase inhibitors by a directed screening approach.
Bioorg Med Chem Lett
; 21(18): 5224-9, 2011 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-21835616
ABSTRACT
A directed screen of a relatively small number of compounds, selected for kinase ATP pocket binding potential, yielded a novel series of hit compounds (1). Hit explosion on two binding residues identified compounds 27 and 43 as the best leads for an optimization program having reduced secondary metabolism, as measured by in vitro rat hepatocytes incubation, leading to oral bio-availability. Structure-activity relationships and molecular modeling have suggested a binding mode for the most potent inhibitor 12.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Proteínas Proto-Oncogênicas c-met
/
Inibidores de Proteínas Quinases
/
Descoberta de Drogas
/
Anilidas
Tipo de estudo:
Diagnostic_studies
/
Prognostic_studies
/
Screening_studies
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Reino Unido