Title of article
Discovery of a potent and selective αvβ3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model
Author/Authors
Seiji Iwama، نويسنده , , Tomoko Kitano، نويسنده , , Fumiyo Fukuya، نويسنده , , Yayoi Honda، نويسنده , , Yuji Sato and Hiromitsu Ishii، نويسنده , , Mitsue Notake، نويسنده , , Toshiya Morie، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
2567
To page
2570
Abstract
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.
Keywords
fax: +81-663387656 , e-mail: seiji-iwama@dainippon-pharm.co.jp , Integrin rat balloon model.* Corresponding author. Tel.: +81-663375901
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794439
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