Krishnaiah, Maddeboina published the artcileSynthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase, Name: [1,2,4]Triazolo[1,5-a]pyridine-6-carbaldehyde, the main research area is triazolopyridinylimidazole pyridinyl preparation transforming growth factor kinase inhibitor; ALK5 inhibitor; Cancer; Fibrosis; Kinase assay; TGF-β.
To further optimize a clin. candidate (EW-7197), a series of 5-(3-, 4-, or 5-fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles have been synthesized and evaluated for their TGF-β type I receptor kinase (ALK5) and p38α MAP kinase inhibitory activity in an enzyme assay. The 5-(5-fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles displayed a level of potency similar to that of EW-7197 against both ALK5 (IC50 = 7.68-13.70 nM) and p38α MAP kinase (IC50 = 1240-3370 nM). Among them, I inhibited ALK5 with IC50 value of 7.68 nM in a kinase assay and displayed 82% inhibition at 100 nM in a luciferase reporter assay.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 614750-81-1 belongs to class pyridine-derivatives, name is [1,2,4]Triazolo[1,5-a]pyridine-6-carbaldehyde, and the molecular formula is C7H5N3O, Name: [1,2,4]Triazolo[1,5-a]pyridine-6-carbaldehyde.