SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Bioorg Med Chem Lett
; 20(5): 1744-8, 2010 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-20153189
ABSTRACT
The SAR of PXR transactivation by 3-(benzimidazol-2-yl)-pyridine-2-one based ATP competitive inhibitors of Insulin-like Growth Factor 1 Receptor kinase (IGF-1R) is discussed. Compounds without PXR transactivation, with in vivo antitumor activity, reduced protein binding and improved oral exposure are presented.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzimidazóis
/
Receptores de Esteroides
/
Ativação Transcricional
/
Receptor IGF Tipo 1
/
Inibidores de Proteínas Quinases
/
Antineoplásicos
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article