Discovery of a potent and selective αvβ3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model

A new series of phenylpiperazine-based derivatives with strong antagonistic activity for αvβ3 integrin were synthesized. Of these derivatives, the fluorine-substituted compound 8 showed strong inhibitory activity and high selectivity for αvβ3 integrin receptor (IC50 = 0.055 nM). In vivo evaluation of the antistenotic effects of 8 indicated that this compound significantly inhibits neointima formation in rat balloon injury model.