AI Article Synopsis
- A range of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles has been synthesized and tested for their ability to inhibit the ALK5 enzyme.
- Compound 14n demonstrated strong inhibitory effectiveness with an IC(50) value of 0.57 nM, making it a potent candidate.
- Additionally, it achieved 94% inhibition in a luciferase reporter assay in specific cell lines, indicating high potential for further research and development.
Article Abstract
A series of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles 14a-ae, 16a, 16b, and 21a-c has been prepared and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(4-methoxyphenyl)-3-(6-methylpyridin-2-yl)-1H-pyrazole-1-carbothioamide (14n) inhibited ALK5 phosphorylation with IC(50) value of 0.57 nM and showed 94% inhibition at 100 nM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.
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| http://dx.doi.org/10.1016/j.bmcl.2011.08.064 | DOI Listing |
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