Biological evaluation of new largazole analogues: Alteration of macrocyclic scaffold with click chemistry

Xianlin Li, Zhenchao Tu, Hua Li, Chunping Liu, Zheng Li, Qiao Sun, Yiwu Yao, Jinsong Liu, Sheng Jiang

Research output: Contribution to journalArticlepeer-review

31 Scopus citations

Abstract

We report the design, synthesis, and biological evaluation of a new series of largazole analogues in which a 4-methylthiazoline moiety was replaced with a triazole and tetrazole ring, respectively. Compound 7 bearing a tetrazole ring was identified to show much better selectivity for HDAC1 over HDAC9 than largazole (10-fold). This work could serve as a foundation for further exploration of selective HDAC inhibitors using a largazole molecular scaffold.

Original languageEnglish (US)
Pages (from-to)132-136
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume4
Issue number1
DOIs
StatePublished - Jan 10 2013

Keywords

  • click chemistry
  • HDAC inhibitor
  • largazole
  • macrocycles
  • peptides

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

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