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. 2014 Dec 1;24(23):5497-501.
doi: 10.1016/j.bmcl.2014.10.019. Epub 2014 Oct 13.

Aurones as histone deacetylase inhibitors: identification of key features

Vincent Zwick  1 , Alkiviadis-Orfefs Chatzivasileiou  2 , Nathalie Deschamps  1 , Marina Roussaki  2 , Claudia A Simões-Pires  1 , Alessandra Nurisso  1 , Iza Denis  3 , Christophe Blanquart  4 , Nadine Martinet  5 , Pierre-Alain Carrupt  1 , Anastasia Detsi  6 , Muriel Cuendet  7
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Aurones as histone deacetylase inhibitors: identification of key features

Vincent Zwick et al. Bioorg Med Chem Lett. .

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: Aurone; Docking; Histone deacetylase; Structure activity relationship.

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