2-Aminoimidazoles inhibitors of TGF-β receptor 1

D Bonafoux, C Chuaqui, PA Boriack-Sjodin…

Index: Bonafoux, Dominique; Chuaqui, Claudio; Boriack-Sjodin, P. Ann; Fitch, Chris; Hankins, Gretchen; Josiah, Serene; Black, Cheryl; Hetu, Gregg; Ling, Leona; Lee, Wen-Cherng Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 912 - 916

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Citation Number: 14

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-βR1. Substitution of the amino group of 3 typically led to a slight decrease in the affinity for the receptor and in TGF-β-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 ...