Design and synthesis of isoquinolines and benzimidazoles as RAF kinase inhibitors.
Bioorg Med Chem Lett
; 21(8): 2264-9, 2011 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-21420298
ABSTRACT
RAF kinase plays a critical role in the RAF-MEK-ERK signaling pathway and inhibitors of RAF could be of use for the treatment of various cancer types. We have designed potent RAF-1 inhibitors bearing novel bicyclic heterocycles as key structural elements for the interaction with the hinge region. In both series exploration of the SAR was focussed on the substitution of the phenyl ring, which binds to the induced fit pocket. Overall, it was confirmed that incorporation of lipophilic substituents was needed for potent Raf inhibition and a number of potent analogues were obtained.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzimidazóis
/
Quinases raf
/
Inibidores de Proteínas Quinases
/
Isoquinolinas
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2011
Tipo de documento:
Article