Solid-phase synthesis of a selective alpha(v)beta(3) integrin antagonist library

被引：65

作者：

Corbett, JW ^{[1
]}

Graciani, NR ^{[1
]}

Mousa, SA ^{[1
]}

DeGrado, WF ^{[1
]}

机构：

[1] UNIV PENN,SCH MED,PHILADELPHIA,PA 19104

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(97)00200-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Solid-phase synthesis was used to generate a focused RGD peptide mimetic library in an effort to identify potent and selective alpha(v) beta(3) 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 alpha(v) beta(3) ELISA assay. (C) 1997 The DuPont Merck Pharmaceutical Company. Published by Elsevier Science Ltd.

引用

页码：1371 / 1376

页数：6

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