期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 12, 页码 3650-3658出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.02.024
关键词
Epigenetics; Histone deacetylase; Enzyme inhibitors; Natural products; Depsipeptide
资金
- Cancer Research UK
- EPSRC
- Southampton Cancer Research UK Centre
- Experimental Cancer Medicine Centre
- COST Action [TD0905]
The total synthesis of largazole and four analogues is reported. All analogues were nanomolar HDAC inhibitors. The antiproliferative activity is driven by lipophilicity and cell permeability. In murine liver homogenates, largazole is rapidly metabolized (half-life <= 5 min) to the thiol which has a half-life of 51 min. (C) 2011 Elsevier Ltd. All rights reserved.
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