期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 2, 页码 605-611出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.12.005
关键词
HDAC inhibitor; Fluoroalkene
资金
- Ministry of Education, Culture, Sports, Science and Technology, Japan
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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