ienz_a_1941920_sm3737.pdf (3.78 MB)
Download file

Ring size changes in the development of class I HDAC inhibitors

Download (3.78 MB)
journal contribution
posted on 2021-06-25, 04:20 authored by Er-Chieh Cho, Chi-Yuan Liu, Di-Wei Tang, Hsueh-Yun Lee

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.

Funding

This research was supported by the Ministry of Science and Technology, Taiwan [grant no. MOST108-2320-B-038-042-MY3 and MOST 109-2320-B-038-038], Taiwan, and WanFang Hospital, Chi-Mei Medical Center, and Hualien Tzu-Chi Hospital Joint Cancer Center Grant-Focus on Colon Cancer Research [MOHW109-TDU-B-212-134020, supported by Health and welfare surcharge of tobacco products], Taiwan.

History