1.
Bioorg Med Chem Lett
; 14(10): 2411-5, 2004 May 17.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15109623
RESUMEN
The discovery and structure-activity relationship of a novel series of coumarin-based TNF-alpha inhibitors is described. Starting from the initial lead 1a, various derivatives were prepared surrounding the coumarin core structure to optimize the in vitro inhibitory activity of TNF-alpha production by human peripheral blood mononuclear cells (hPBMC), stimulated by bacterial lipopolysaccharide (LPS). Selected compounds also demonstrated in vivo inhibition of TNF-alpha production in rats.
Asunto(s)
Cumarinas/síntesis química , Cumarinas/farmacología , Factor de Necrosis Tumoral alfa/antagonistas & inhibidores , Células Cultivadas , Relación Dosis-Respuesta a Droga , Humanos , Concentración 50 Inhibidora , Leucocitos Mononucleares/metabolismo , Lipopolisacáridos/farmacología , Relación Estructura-Actividad , Factor de Necrosis Tumoral alfa/metabolismo
2.