Ring size changes in the development of class I HDAC inhibitors

Er Chieh Cho, Chi Yuan Liu, Di Wei Tang, Hsueh Yun Lee

Research output: Contribution to journalArticlepeer-review

Abstract

Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.

Original languageEnglish
Pages (from-to)1387-1401
Number of pages15
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume36
Issue number1
DOIs
Publication statusPublished - 2021

Keywords

  • colon cancer
  • HDAC
  • ring transformation
  • Thienylbenzamides

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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