1422465-14-2

Upstream product

• 50998-17-9 6-bromoquinoxaline 
• 1224886-20-7 2-methyl-6-(4-phenyl-1H-1,2,3-triazol-1-yl)pyridine 
• 5315-25-3 2-bromo-6-methylpyridine 
• 212182-36-0 2-azido-6-methylpyridine 

Relevant academic research and scientific papers

Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5- (quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-β type 1 receptor kinase inhibitors

A series of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles has been synthesized and evaluated for their ALK5 inhibitory activity. The 1-(6-methylpyridin-2-yl)-1,2,3-triazoles were assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition. Following this, quinoxaline was introduced through Pd-catalyzed direct arylation. The synthesized 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles revealed significant selectivity differences with respect to p38α MAP kinase. In particular, 12k showed 80.8% ALK5 inhibitory activity at a concentration of 10 μM and IC50 value of 4.69 μM, but did not show p38α MAP kinase inhibitory activity (-1.94% inhibition at a concentration of 10 μM).