Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 4, Pages 481-486Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.8b00517
Keywords
Histone deacetylase; HDAC3 selective; nonhydroxamate; nonbenzamide
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Funding
- Italian National Compound and Screening Collection (CNCCS consortium)
- RESEARCH project (Life2020, POR FESR 2014/2020 regione Lazio)
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The application of class I HDAC inhibitors as cancer therapies is well established, but more recently their development for nononcological indications has increased. We report here on the generation of improved class I selective human HDAC inhibitors based on an ethylketone zinc binding group (ZBG) in place of the hydroxamic acid that features the majority of HDAC inhibitors. We also describe a novel set of HDAC3 isoform selective inhibitors that show stronger potency and selectivity than the most commonly used HDAC3 selective tool compound RGFP966. These compounds are again based on an alternative ZBG with respect to the ortho-anilide that is featured in HDAC3 selective compounds reported to date.
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