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Comparative Study
. 2008 Apr 1;18(7):2509-12.
doi: 10.1016/j.bmcl.2007.07.068. Epub 2007 Aug 21.

Selective cell adhesion inhibitors: Barbituric acid based alpha4beta7--MAdCAM inhibitors

Geraldine C Harriman  1 , 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, Michael J Briskin
Affiliations
Comparative Study

Selective cell adhesion inhibitors: Barbituric acid based alpha4beta7--MAdCAM inhibitors

Geraldine C Harriman et al. Bioorg Med Chem Lett. .

Abstract

A novel series of barbituric acid derivatives were identified as selective inhibitors of alpha4beta7 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 alpha4beta1 VCAM.

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