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Aurones as histone deacetylase inhibitors: identification of key features

Chatzivasileiou, Alkiviadis-Orfefs
Deschamps, Nathalie
Roussaki, Marina
Denis, Iza
Blanquart, Christophe
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Published in Bioorganic & medicinal chemistry letters. 2014, vol. 24, no. 23, p. 5497-501
Abstract In this study, a total of 22 flavonoids were tested for their HDAC inhibitory activity using fluorimetric and BRET-based assays. Four aurones were found to be active in both assays and showed IC50 values below 20 μM in the enzymatic assay. Molecular modelling revealed that the presence of hydroxyl groups was responsible for good compound orientation within the isoenzyme catalytic site and zinc chelation.
Keywords Benzofurans/chemistryDrug DesignHistone Deacetylase Inhibitors/chemistryHumansModelsMolecularMolecular Structure
PMID: 25455492
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ZWICK, Vincent et al. Aurones as histone deacetylase inhibitors: identification of key features. In: Bioorganic & medicinal chemistry letters, 2014, vol. 24, n° 23, p. 5497-501. doi: 10.1016/j.bmcl.2014.10.019 https://archive-ouverte.unige.ch/unige:95051

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Deposited on : 2017-06-26

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