Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists.
Bioorg Med Chem Lett
; 14(6): 1471-6, 2004 Mar 22.
Article
em En
| MEDLINE
| ID: mdl-15006384
ABSTRACT
We describe a series of conformationally-restricted cinnamic acid peptidomimetics as well as several cinnamic acid isosteres, including 3-phenylpropionic acids, 2-amino-3-phenylpropionic acids, phenoxyacetic acids and 2-phenylcyclopropylcarboxylic acids. Several analogues demonstrated low to sub-nanomolar potencies against alpha(v)beta(3) and greater than 200-fold selectivity against the other beta(3) integrin alpha(IIb)beta(3). In whole 293 cells, many of these analogues also showed modest selectivity against other alpha(v) integrins such as alpha(v)beta(1) and alpha(v)beta(5). These compounds were synthesized from readily available starting materials using either Heck or Mitsunobu coupling conditions.
Buscar no Google
Base de dados:
MEDLINE
Assunto principal:
Cinamatos
/
Integrina alfaVbeta3
Idioma:
En
Ano de publicação:
2004
Tipo de documento:
Article