| Literature DB >> 19135364 |
Dominique Bonafoux1, Claudio Chuaqui, P Ann Boriack-Sjodin, Chris Fitch, Gretchen Hankins, Serene Josiah, Cheryl Black, Gregg Hetu, Leona Ling, Wen-Cherng Lee.
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.Entities:
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Year: 2008 PMID： 19135364 DOI： 10.1016/j.bmcl.2008.11.119
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823