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Satoshi Osada

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Organization: Saga University
Department: Department of Chemistry and Applied Chemistry, Faculty of Science and Engineering
Title:
Fluoroalkene modification of mercaptoacetamide-based histone deacetylase inhibitors
Co-reporter:Satoshi Osada, Satoshi Sano, Mariko Ueyama, Yoshiro Chuman, Hiroaki Kodama, Kazuyasu Sakaguchi
Bioorganic & Medicinal Chemistry 2010 Volume 18(Issue 2) pp:605-611
Publication Date(Web):15 January 2010
DOI:10.1016/j.bmc.2009.12.005
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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