| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375684 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
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 pharmacokinetic profile.
Graphical abstractAcylated 2-amidoimidazoles were identified as potent and selective inhibitor of TGF-βR1 that offer a superior pharmacokinetic profile compared to unsubstituted or alkylated 2-aminoimidazoles.Figure optionsDownload full-size imageDownload as PowerPoint slide
