Bioorganic and Medicinal Chemistry Letters p. 2567 - 2570 (2004)
Update date:2022-08-03
Topics:
Iwama, Seiji
Kitano, Tomoko
Fukuya, Fumiyo
Honda, Yayoi
Sato, Yuji
Notake, Mitsue
Morie, Toshiya
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 αvβ 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.
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