Solid-phase synthesis of a nonpeptide RGD mimetic library: new selective αvβ3 integrin antagonists

GAG Sulyok, C Gibson, SL Goodman…

Index: Sulyok; Gibson; Goodman; Hoelzemann; Wiesner; Kessler Journal of Medicinal Chemistry, 2001 , vol. 44, # 12 p. 1938 - 1950

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Citation Number: 130

Abstract

The solid-phase synthesis of a low molecular weight RGD mimetic library is described. Activities of the compounds in inhibiting the interaction of ligands, vitronectin and fibrinogen, with isolated immobilized integrins αvβ3 and αIIbβ3 were determined in a screening assay. Highly active and selective nonpeptide αvβ3 integrin antagonists with regard to orally bioavailability were developed, based on the aza-glycine containing lead compound 1. An ...