Synthesis and biological evaluation of novel 2-pyridinyl-[1,2,3]triazoles as inhibitors of transforming growth factor β1 type 1 receptor

Dae Kee Kim, Joonseop Kim, Hyun Ju Park

Research output: Contribution to journalArticlepeer-review

85 Scopus citations

Abstract

A series of 2-pyridinyl-[1,2,3]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 8d showed significant ALK5 inhibition (SBE-luciferase activity, 25%; p3TP-luciferase activity, 17%) at a concentration of 5μM that is comparable to that of SB-431542 (SBE-luciferase activity, 21%; p3TP-luciferase activity, 12%), but weak p38α MAP kinase inhibition (13%) at a concentration of 10μM that is much lower than that of SB-431542 (54%).

Original languageEnglish
Pages (from-to)2401-2405
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number10
DOIs
StatePublished - 17 May 2004

Keywords

  • 2-Pyridinyl-[1,2,3]triazoles
  • ALK5
  • Inhibitors
  • TGF-β1 type 1 receptor

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