期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 14, 页码 5219-5228出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.05.042
关键词
HDAC inhibitors; Molecular docking; Caffeic acid derivatives; Chlorogenic acid; Curcumin; Carboxylic acid derivatives
资金
- The Scientific and Technological Research Council of Turkey [105G014]
In the light of known HDAC inhibitors, 33 carboxylic acid derivatives were tested to understand the structural requirements for HDAC inhibition activity. Several modifications were applied to develop the structure-activity relationships of carboxylic acid HDAC inhibitors. HDAC inhibition activities were investigated in vitro by using HeLa nuclear extract in a fluorimetric assay. Molecular docking was also carried out for the human HDAC8 enzyme in order to predict inhibition activity and the 3D poses of inhibitor-enzyme complexes. Of these compounds, caffeic acid derivatives such as chlorogenic acid and curcumin were found to be highly potent compared to sodium butyrate, which is a well-known HDAC inhibitor. (C) 2009 Elsevier Ltd. All rights reserved.
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