Design, synthesis, and biological evaluation of novel 2-pyridinyl-[1,2,4] 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

23 Scopus citations

Abstract

A series of 2-pyridinyl-[1,2,4]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 12b showed significant ALK5 inhibition (SBE-Luciferase, 73%; p3TP-Luciferase, 85%) at a concentration of 5μM that is comparable to that of SB-431542 (SBE-Luciferase, 79%; p3TP-Luciferase, 88%), but weak p38α MAP kinase inhibition (4%) at a concentration of 10μM that is much lower than that of SB-431542 (54%). The binding mode of 12b generated by flexible docking studies revealed that the structure of 12b is a good fit into the (NPC-30345)-binding cavity of ALK5.

Original languageEnglish
Pages (from-to)2013-2020
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume12
Issue number9
DOIs
StatePublished - 1 May 2004

Keywords

  • 2-Pyridinyl-[1,2,4]triazoles
  • ALK5
  • Inhibitors
  • TGF-β1 type 1 receptor

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