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Updated: Jun 17, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Fluoroalkene modification of mercaptoacetamide-based histone deacetylase inhibitors
Satoshi Osada1, Satoshi Sano, Mariko Ueyama
1Department of Chemistry and Applied Chemistry, Faculty of Science and Engineering, Saga University, 1 Honjo, Saga 840-8502, Japan. osadas@cc.saga-u.ac.jp
Abstract:
Inhibitors of histone deacetylases (HDAC) are emerging as a promising class of anti-cancer agents. The mercaptoacetoamide-based inhibitors are reported to be less toxic than hydroxamate and are worthy of further consideration. Therefore, we have designed a series of analogs as potential inhibitors of HDACs, in which the mercaptoacetamide group was replaced by (mercaptomethyl)fluoroalkene, and their HDAC inhibitory activity was evaluated. Subnanomolar inhibition was observed for all synthetic compounds.
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