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
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| 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
Banco de datos:
MEDLINE
Asunto principal:
Pirroles
/
Triazinas
/
Proteína Quinasa 14 Activada por Mitógenos
/
Inhibidores de Proteínas Quinasas
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Año:
2008
Tipo del documento:
Article