4.7 Article

Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies

期刊

BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 14, 页码 5219-5228

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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

  1. The Scientific and Technological Research Council of Turkey [105G014]

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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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