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

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Molecular modifications on carboxylic acid derivatives as potent histonedeacetylase inhibitors Activity and docking studies.pdf (4.678Mb)
Date
2009
Author
Bora-Tatar, Gamze
Dayangac-Erden, Didem
Demir, Ayhan S.
Dalkara, Sevim
Yelekçi, Kemal
Erdem-Yurter, Hayat
Abstract
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.

Source

Bioorganic & Medicinal Chemistry

Issue

14

Volume

17

Pages

5219-5228

URI

https://hdl.handle.net/20.500.12469/1096
https://doi.org/10.1016/j.bmc.2009.05.042

Collections

  • Araştırma Çıktıları / Scopus [1565]
  • Araştırma Çıktıları / WOS [1518]
  • Biyoinformatik ve Genetik / Bioinformatics and Genetics [220]

Keywords

HDAC inhibitors
Molecular docking
Caffeic acid derivatives
Chlorogenic acid
Curcumin
Carboxylic acid derivatives

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