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Bioorg Med Chem Lett. 2009 Feb 1;19(3):912-6. doi: 10.1016/j.bmcl.2008.11.119. Epub 2008 Dec 11.

2-Aminoimidazoles inhibitors of TGF-beta receptor 1.

Author information

1
Abbot Laboratories, 381 Plantation Street, Worcester, MA 01605-2323, USA. dominique.bonafoux@abbott.com

Abstract

The 4-(5-fluoro-6-methyl-pyridin-2-yl)-5-quinoxalin-6-yl-1H-imidazol-2-ylamine 3 is a potent and selective inhibitor of TGF-betaR1. Substitution of the amino group of 3 typically led to a slight decrease in the affinity for the receptor and in TGF-beta-inducted PAI-luciferase reporter activity. However, 2-acetamidoimidazoles were identified as attractive candidates for further optimization as a result of their significant activity combined to their superior pharmacokinetic profile.

PMID:
19135364
DOI:
10.1016/j.bmcl.2008.11.119
[Indexed for MEDLINE]

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