Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.
Bioorg Med Chem Lett
; 23(8): 2306-12, 2013 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-23489628
ABSTRACT
The V600E BRAF kinase mutation, which activates the downstream MAPK signaling pathway, commonly occurs in about 8% of all human malignancies and about 50% of all melanomas. In this study, we employed virtual screening and chemical synthesis to identify a series of N-(thiophen-2-yl) benzamide derivatives as potent BRAF(V600E) inhibitors. Structure-activity relationship studies of these derivatives revealed that compounds b40 and b47 are the two most potent BRAF(V600E) inhibitors in this series.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Benzamidas
/
Proteínas Proto-Oncogênicas B-raf
Tipo de estudo:
Diagnostic_studies
Limite:
Humans
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article