Ring size changes in the development of class I HDAC inhibitors

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

研究成果: 雜誌貢獻文章同行評審

摘要

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.

原文英語
頁(從 - 到)1387-1401
頁數15
期刊Journal of Enzyme Inhibition and Medicinal Chemistry
36
發行號1
DOIs
出版狀態已發佈 - 2021

ASJC Scopus subject areas

  • 藥理
  • 藥物發現

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