Ring size changes in the development of class I HDAC inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry

Er-Chieh Cho¹  Chi-Yuan Liu¹  Hsueh-Yun Lee¹  Di-Wei Tang¹ 

[1] School of Pharmacy, College of Pharmacy, Taipei Medical University;

关键词: thienylbenzamides;    ring transformation;    hdac;    colon cancer;   

DOI  :  10.1080/14756366.2021.1941920

来源: DOAJ

【 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.

【 授权许可】

Unknown