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

Bioorganic & Medicinal Chemistry Letters
Purushottam M Dewang, Dae-Kee Kim

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 microM in luciferase reporter assays using HaCaT cells transiently transfected with p3TP-luc reporter construct and ARE-luc reporter construct, respectively.

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Citations

Aug 3, 2011·Chemical Reviews·Santos FusteroAntonio Simón-Fuentes
Feb 19, 2015·Journal of Enzyme Inhibition and Medicinal Chemistry·Marisa CabezaEugene Bratoeff
Mar 19, 2016·The Journal of Organic Chemistry·Krystyna DemkiwLei Zhu
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Jun 7, 2013·Medicinal Research Reviews·Ling ZhangCheng-He Zhou
Dec 24, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Li-Min ZhaoCheng Hua Jin
Feb 17, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Asad UllahSyed Lal Badshah
Nov 12, 2021·Chemistry : a European Journal·Anton Kudashev, Olivier Baudoin

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