2. Academic Validation
  3. Fluoroalkene modification of mercaptoacetamide-based histone deacetylase inhibitors

Fluoroalkene modification of mercaptoacetamide-based histone deacetylase inhibitors

  • Bioorg Med Chem. 2010 Jan 15;18(2):605-11. doi: 10.1016/j.bmc.2009.12.005.
Satoshi Osada 1,  Satoshi Sano,  Mariko Ueyama,  Yoshiro Chuman,  Hiroaki Kodama,  Kazuyasu Sakaguchi
Affiliations

Affiliation

  • 1 Department of Chemistry and Applied Chemistry, Faculty of Science and Engineering, Saga University, 1 Honjo, Saga 840-8502, Japan. osadas@cc.saga-u.ac.jp
PMID: 20036560 DOI: 10.1016/j.bmc.2009.12.005
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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