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Identification of mercaptoacetamide-based HDAC6 inhibitors via a lean inhibitor strategy : screening, synthesis, and biological evaluation
- Source :
- CHEMICAL COMMUNICATIONS
- Publication Year :
- 2022
-
Abstract
- Non-selective inhibition of different histone deacetylase enzymes by hydroxamic acid-based drugs causes severe side effects when used as a (long-term) cancer treatment. In this work, we searched for a potent zinc-binding group able to replace the contested hydroxamic acid by employing a lean inhibitor strategy. This instructed the synthesis of a set of HDAC6-selective inhibitors containing the more desirable mercaptoacetamide moiety. Biological evaluation of these new compounds showed an IC50 in the nanomolar range, dose-dependent HDAC6 inhibition in MM1.S cells and improved genotoxicity results, rendering these new inhibitors valuable hits for applications even beyond oncology.
Details
- Language :
- English
- ISSN :
- 13597345 and 1364548X
- Database :
- OpenAIRE
- Journal :
- CHEMICAL COMMUNICATIONS
- Accession number :
- edsair.doi.dedup.....df6dcc9f7744217d7d1e8e784425ff96