Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 2, Pages 605-611Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.12.005
Keywords
HDAC inhibitor; Fluoroalkene
Funding
- Ministry of Education, Culture, Sports, Science and Technology, Japan
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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. (C) 2009 Elsevier Ltd. All rights reserved.
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