Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors

Doohee Song, Yunjeong Park, Jieun Yoon, Waqar Aman, Jung Mi Hah, Jae Sang Ryu

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

A series of 1,2,3-triazolylsalicylamide derivatives has been developed from the antiproliferative agent 7 and was evaluated for their Aurora kinase inhibitory activity. The novel 1,2,3-triazolylsalicylamide scaffold could be readily assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition, allowing rapid access to the structurally diverse analogues. The synthesized 1,2,3-triazolylsalicylamide derivatives revealed a significant Aurora kinase inhibitory activity. In particular, 8g inhibited Aurora A with IC50 values of 0.37 μM. The critical role of phenolic -OH in the binding was confirmed by a molecular modeling study.

Original languageEnglish
Pages (from-to)4855-4866
Number of pages12
JournalBioorganic and Medicinal Chemistry
Volume22
Issue number17
DOIs
StatePublished - 1 Sep 2014

Keywords

  • 1,2,3-Triazole
  • Anticancer
  • Aurora kinase
  • Click chemistry
  • Library

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