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

Article abstract of DOI:10.1016/j.bmcl.2004.02.075

A new series of phenylpiperazine-based derivatives with strong antagonistic activity for α_vβ₃ integrin were synthesized. Of these derivatives, the fluorine-substituted compound 8 showed strong inhibitory activity and high selectivity for α_vβ ₃ integrin receptor (IC₅₀=0.055nM). In vivo evaluation of the antistenotic effects of 8 indicated that this compound significantly inhibits neointima formation in rat balloon injury model.