Solid-phase synthesis of a selective αvβ3 integrin antagonist library

Solid-phase synthesis was used to generate a focused RGD peptide mimetic library in an effort to identify potent and selective αvβ3 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 αvβ3 ELISA assay.