The development of new bicyclic pyrazole-based cytokine synthesis inhibitors.
Bioorg Med Chem Lett
; 14(19): 4945-8, 2004 Oct 04.
Article
en En
| MEDLINE
| ID: mdl-15341957
ABSTRACT
4-Aryl-5-pyrimidyl-based cytokine synthesis inhibitors of TNF-alpha production, which contain a novel bicyclic pyrazole heterocyclic core, are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-alpha production in a THP-1 cell-based assay and against human p38 alpha MAP kinase in an isolated enzyme assay. The X-ray crystal structure of a bicyclic pyrazole inhibitor co-crystallized with mutated p38 (mp38) is presented.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirazoles
/
Factor de Necrosis Tumoral alfa
/
Proteínas Quinasas p38 Activadas por Mitógenos
/
Inhibidores Enzimáticos
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
Estados Unidos