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Ring size changes in the development of class I HDAC inhibitors.

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.

SUBMITTER: Cho EC

PROVIDER: S-EPMC8231390 | biostudies-literature |

REPOSITORIES: biostudies-literature

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