Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.
Bioorg Med Chem Lett
; 17(18): 5019-24, 2007 Sep 15.
Article
en En
| MEDLINE
| ID: mdl-17664068
ABSTRACT
The synthesis and structure-activity relationships (SAR) of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to the identification of compound (21) as a potent inhibitor of p38alpha MAP kinase with good cellular potency toward the inhibition of TNF-alpha production. X-ray co-crystallography of an oxalamide analog (24) bound to unphosphorylated p38alpha is also disclosed.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Compuestos Bicíclicos con Puentes
/
Proteínas Quinasas p38 Activadas por Mitógenos
/
Inhibidores de Proteínas Quinasas
/
Compuestos Heterocíclicos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2007
Tipo del documento:
Article
País de afiliación:
Estados Unidos