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 language | English |
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Pages (from-to) | 1387-1401 |
Number of pages | 15 |
Journal | Journal of Enzyme Inhibition and Medicinal Chemistry |
Volume | 36 |
Issue number | 1 |
DOIs | |
Publication status | Published - 2021 |
Keywords
- colon cancer
- HDAC
- ring transformation
- Thienylbenzamides
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery