1.
Bioorg Med Chem Lett
; 16(4): 839-44, 2006 Feb 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16298127
RESUMEN
We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(v)beta3 and, in addition, show selectivity relative to the other beta3 integrin alpha(IIb)beta3. In whole cells, the majority of these analogs also demonstrated modest selectivity against other alpha(v) integrins such as alpha(v)beta1 and alpha(v)beta6.
Asunto(s)
Butiratos/síntesis química , Butiratos/farmacología , Integrina alfaVbeta3/antagonistas & inhibidores , Oxadiazoles/síntesis química , Oxadiazoles/farmacología , Antígenos de Neoplasias , Butiratos/química , Línea Celular , Humanos , Integrinas/antagonistas & inhibidores , Estructura Molecular , Oxadiazoles/química , Receptores de Vitronectina/antagonistas & inhibidores , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 15(1): 93-8, 2005 Jan 03.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15582418
RESUMEN
A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.