Aurones as histone deacetylase inhibitors: identification of key features

Zwick, Vincent; Chatzivasileiou, Alkiviadis-Orfefs; Deschamps, Nathalie; Roussaki, Marina; Simoes Avello, Claudia; Nurisso, Alessandra; Denis, Iza; Blanquart, Christophe; Martinet, Nadine; Carrupt, Pierre-Alain; Detsi, Anastasia; Cuendet, Muriel

doi:10.1016/j.bmcl.2014.10.019

Scientific article

English

Aurones as histone deacetylase inhibitors: identification of key features

ContributorsZwick, Vincent; Chatzivasileiou, Alkiviadis-Orfefs; Deschamps, Nathalie; Roussaki, Marina; Simoes Avello, Claudia; Nurisso, Alessandra; Denis, Iza; Blanquart, Christophe; Martinet, Nadine; Carrupt, Pierre-Alain; Detsi, Anastasia; Cuendet, Muriel

Published inBioorganic & medicinal chemistry letters, vol. 24, no. 23, p. 5497-5501

Publication date2014

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/chemistry
Drug Design
Histone Deacetylase Inhibitors/chemistry
Humans
Models
Molecular
Molecular Structure

Affiliation entities

Faculté des sciences / Section des sciences pharmaceutiques

Citation (ISO format)

ZWICK, Vincent et al. Aurones as histone deacetylase inhibitors: identification of key features. In: Bioorganic & medicinal chemistry letters, 2014, vol. 24, n° 23, p. 5497–5501. doi: 10.1016/j.bmcl.2014.10.019

Article (Published version)

Identifiers

PID : unige:95051
DOI : 10.1016/j.bmcl.2014.10.019
PMID : 25455492

Journal ISSN0960-894X

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Aurones as histone deacetylase inhibitors: identification of key features

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