Bioorganic & medicinal chemistry letters

Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors

PM Dewang, DK Kim

Index: Dewang, Purushottam M.; Kim, Dae-Kee Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 14 p. 4228 - 4232

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Citation Number: 21

Abstract

A series of 2-pyridyl-substituted pyrazoles (16a–d, 17, 18, and 28a–e) and imidazoles (22 and 23) has been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 3-(3-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)-1H- pyrazole-1-carbothioamido) benzamide (28c) showed 96% and 93% inhibition at 0.1 μM in luciferase reporter assays using HaCaT cells transiently transfected with p3TP-luc reporter ...