Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors

Yunkyung Jeong, Jooyeon Lee, Jae Sang Ryu

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

A series of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives were designed, synthesized, and evaluated for the Aurora kinase inhibitory activities. The novel hinge-binder tethered 1,2,3-triazolylsalicylamide scaffold was effectively assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC). A variety of alkynes with hinge binders were used to search proper structures-binding relationship to the hinge region. The synthesized 1,2,3-triazolylsalicylamide derivatives showed significant Aurora kinase inhibitory activity. In particular, 8a inhibited Aurora A kinase with an IC50 value of 0.284 μM, whereas 8m inhibited Aurora B kinase with an IC50 value of 0.364 μM.

Original languageEnglish
Pages (from-to)2114-2124
Number of pages11
JournalBioorganic and Medicinal Chemistry
Volume24
Issue number9
DOIs
StatePublished - 1 May 2016

Keywords

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

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