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

Purushottam M. Dewang, Dae Kee Kim

Research output: Contribution to journalArticlepeer-review

28 Scopus citations

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 construct and ARE-luc reporter construct, respectively.

Original languageEnglish
Pages (from-to)4228-4232
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number14
DOIs
StatePublished - 15 Jul 2010

Keywords

  • ALK5 inhibitor
  • Cell-based luciferase reporter assays
  • TGF-β

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