Convergent, parallel synthesis of a series of β-substituted 1,2,4-oxadiazole butanoic acids as potent and selective αvβ3 receptor antagonists

被引：41

作者：

Boys, ML

Schretzman, LA

Chandrakumar, NS

Tollefson, MB

Mohler, SB

Downs, VL

Penning, TD

Russell, MA

Wendt, JA

Chen, BB

Stenmark, HG

Wu, HW

Spangler, DP

Clare, M

Desai, BN

Khanna, IK

Nguyen, MN

Duffin, T

Engleman, VW

Finn, MB

Freeman, SK

Hanneke, ML

Keene, JL

Klover, JA

Nickols, GA

Nickols, MA

Steininger, CN

Westlin, M

Westlin, W

Yu, YX

Wang, YP

Dalton, CR

Norring, SA

机构：

[1] PfizerGlobal Res & Dev, Dept Chem, Ann Arbor, MI 48105 USA

[2] PfizerGlobal Res & Dev, Dept Med Chem, Skokie, IL 60077 USA

[3] PfizerGlobal Res & Dev, Dept Med Chem, Chesterfield, MO 63198 USA

[4] PfizerGlobal Res & Dev, Dept Discovery Pharmacol, Chesterfield, MO 63198 USA

[5] PfizerGlobal Res & Dev, Dept Oncol, Chesterfield, MO 63198 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 04期

关键词：

integrin; vitronectin; alpha(v)beta(3); antagonist; 1,2,4-oxadiazole; RGD; peptidomimetic;

D O I：

10.1016/j.bmcl.2005.11.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(V)beta(3) and, in addition, show selectivity relative to the other beta(3) integrin alpha(IIB)beta(3). In whole cells, the majority of these analogs also demonstrated modest selectivity against other alpha(V), integrins such as alpha(V)beta(1) and alpha(V)beta(6). (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：839 / 844

页数：6

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