Ring size changes in the development of class I HDAC inhibitors

Ring size changes in the development of class I HDAC inhibitors

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 HCT1...

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Bibliographic Details
Main Authors: Er-Chieh Cho, Chi-Yuan Liu, Di-Wei Tang, Hsueh-Yun Lee
Format: Article
Language:English
Published: Taylor & Francis Group 2021-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
thienylbenzamides
ring transformation
hdac
colon cancer
Online Access:http://dx.doi.org/10.1080/14756366.2021.1941920
Description
Summary: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.
ISSN:1475-6366
1475-6374

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