Solid-phase synthesis of a selective alpha(v)beta(3) integrin antagonist library

[摘要] Solid-phase synthesis was used to generate a focused RGD peptide mimetic library in an effort to identify potent and selective alpha(v) beta(3) integrin antagonists. Increased activity was observed for compounds possessing a urea linkage to piperazine, with the most active compound (28) exhibiting an IC50 = 1.1 nM in an alpha(v) beta(3) ELISA assay. (C) 1997 The DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd.

[发布日期] 1997-06-03