ienz_a_1941920_sm3737.pdf (3.78 MB)
Ring size changes in the development of class I HDAC inhibitors
journal contribution
posted on 2021-06-25, 04:20 authored by Er-Chieh Cho, Chi-Yuan Liu, Di-Wei Tang, Hsueh-Yun LeeFive 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.