Abstract
A series of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4] triazolo[1,5-a]pyridin-6-yl)thiazoles 12a-ab, 13a, 13b, and 18a-d has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The N-(3-fluorobenzyl)-4-(6- methylpyridin-2-yl)-5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)thiazol-2-amine (12b) inhibited ALK5 phosphorylation with an IC50 value of 7.01 nM and showed 61% inhibition at 30 nM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.
Original language | English |
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Pages (from-to) | 74-84 |
Number of pages | 11 |
Journal | European Journal of Medicinal Chemistry |
Volume | 57 |
DOIs | |
State | Published - Nov 2012 |
Bibliographical note
Funding Information:This work was supported by a grant from Ministry of Education, Science and Technology, Korea ( 20100029596 ).
Keywords
- ALK5 inhibitor
- Cancer
- Cell-based luciferase reporter assay
- Docking
- Fibrosis
- Kinase assay
- TGF-β