Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin- 2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Cheng Hua Jin, Maddeboina Krishnaiah, Domalapally Sreenu, Kota Sudhakar Rao, Vura Bala Subrahmanyam, Chul Yong Park, Jee Yeon Son, Yhun Yhong Sheen, Dae Kee Kim

Research output: Contribution to journalArticlepeer-review

30 Scopus citations

Abstract

A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl) pyrazoles 14a-e, 15a-e, 17a-c, and 18a-d have been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 6-quinolinyl pyrazole analogue 14b inhibited ALK5 phosphorylation with IC50 value of 0.022 μM and showed 84% inhibition at 0.1 μM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.

Original languageEnglish
Pages (from-to)2633-2640
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume19
Issue number8
DOIs
StatePublished - 15 Apr 2011

Bibliographical note

Funding Information:
This work was supported by RP-Grant 2009 of Ewha Womans University.

Keywords

  • ALK5 inhibitor
  • Cancer
  • Cell-based luciferase reporter assay
  • Fibrosis
  • Kinase assay
  • TGF-β

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