Bioorganic & medicinal chemistry letters

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

F Li, Y Park, JM Hah, JS Ryu

Index: Li, Fei; Park, Yunjeong; Hah, Jung-Mi; Ryu, Jae-Sang Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 4 p. 1083 - 1086

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Citation Number: 14

Abstract

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 ...