Selective cell adhesion inhibitors: Barbituric acid based α4β7—MAdCAM inhibitors
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- 作者：Geraldine C. Harriman ; Matthias Brewer ; Robert Bennett ; Cyrille Kuhn ; Marc Bazin ; Greg Larosa ; Paul Skerker ; Nancy Cochran ; Debra Gallant ; Deborah Baxter ; Dominic Picarella ; Bruce Jaffee ; Jay R. Luly
- 关键词：Integrin ; Cell adhesion molecule ; MAdCAM ;
; //www.sciencedirect.com/scidirimg/entities/204e.gif"" alt=""greek small letter alpha"" title=""greek small letter alpha"" border=""0"">4β ; 7 ; Barbituric acid
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：1 April 2008
- 年：2008
- 卷：18
- 期：7
- 页码：2509-2512
- 全文大小：115 K
文摘
A novel series of barbituric acid derivatives were identified as selective inhibitors of ![]()
4β7 MAdCAM (mucosal addressin cell adhesion molecule-1) interactions via a high throughput screening exercise. These inhibitors were optimized to submicromolar potencies in whole cell adhesion assays, retaining their selectivity over ![]()
4β1 VCAM.