Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.
Bioorg Med Chem Lett
; 18(8): 2739-44, 2008 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-18364256
ABSTRACT
A novel series of compounds based on the pyrrolo[2,1-f][1,2,4]triazine ring system have been identified as potent p38 alpha MAP kinase inhibitors. The synthesis, structure-activity relationships (SAR), and in vivo activity of selected analogs from this class of inhibitors are reported. Additional studies based on X-ray co-crystallography have revealed that one of the potent inhibitors from this series binds to the DFG-out conformation of the p38 alpha enzyme.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Triazinas
/
Proteína Quinase 14 Ativada por Mitógeno
/
Inibidores de Proteínas Quinases
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article