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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 | 2021 Dec

REPOSITORIES: biostudies-literature

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

Cho Er-Chieh EC Liu Chi-Yuan CY Tang Di-Wei DW Lee Hsueh-Yun HY

Journal of enzyme inhibition and medicinal chemistry 20211201 1

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. ...[more]

PMID: 34167419

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