A series of 5-(pyridin-2-yl)thiazoles (14a-l and 15a-l) has been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 3-[[5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)thiazol-2-ylamino]methyl ]benzamide (15i) and 3-[[5-(6-ethylpyridin-2-yl)-4-(quinoxalin-6-yl)thiazol-2-ylamino]methyl] benzamide (15k) showed more than 95% inhibition at 0.1 μM in luciferase reporter assays using HaCaT cells transiently transfected with p3TP-luc reporter construct and ARE-luciferase reporter construct.
Bibliographical noteFunding Information:
This work was supported in part by the grants from Ministry of Commerce, Industry and Energy, Korea (M1-0310-43-0001 and M1-0310-43-0002).
- ALK5 inhibitors
- Transforming growth factor-β (TGF-β)