1.
Bioorg Med Chem Lett
; 16(4): 839-44, 2006 Feb 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16298127
RESUMO
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.
Assuntos
Butiratos/síntese química , Butiratos/farmacologia , Integrina alfaVbeta3/antagonistas & inibidores , Oxidiazóis/síntese química , Oxidiazóis/farmacologia , Antígenos de Neoplasias , Butiratos/química , Linhagem Celular , Humanos , Integrinas/antagonistas & inibidores , Estrutura Molecular , Oxidiazóis/química , Receptores de Vitronectina/antagonistas & inibidores , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 15(1): 93-8, 2005 Jan 03.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15582418
RESUMO
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.