Literature DB >> 25455492

Aurones as histone deacetylase inhibitors: identification of key features.

Vincent Zwick1, Alkiviadis-Orfefs Chatzivasileiou2, Nathalie Deschamps1, Marina Roussaki2, Claudia A Simões-Pires1, Alessandra Nurisso1, Iza Denis3, Christophe Blanquart4, Nadine Martinet5, Pierre-Alain Carrupt1, Anastasia Detsi6, Muriel Cuendet7.   

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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh：

Substances：

Year:  2014        PMID： 25455492     DOI： 10.1016/j.bmcl.2014.10.019

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Cellular analysis of the action of epigenetic drugs and probes.

Authors:  Mirjam Hau; Fides Zenk; A Ganesan; Nicola Iovino; Manfred Jung
Journal:  Epigenetics       Date:  2017-01-10       Impact factor: 4.528

2.  2-Benzylidenebenzofuran-3(2H)-ones as a new class of alkaline phosphatase inhibitors: synthesis, SAR analysis, enzyme inhibitory kinetics and computational studies.

Authors:  Jamshaid Ashraf; Ehsan Ullah Mughal; Reem I Alsantali; Amina Sadiq; Rabab S Jassas; Nafeesa Naeem; Zaman Ashraf; Yasir Nazir; Muhammad Naveed Zafar; Amara Mumtaz; Masoud Mirzaei; Satar Saberi; Saleh A Ahmed
Journal:  RSC Adv       Date:  2021-10-29       Impact factor: 4.036

3.  A Rational Approach for the Identification of Non-Hydroxamate HDAC6-Selective Inhibitors.

Authors:  Laura Goracci; Nathalie Deschamps; Giuseppe Marco Randazzo; Charlotte Petit; Carolina Dos Santos Passos; Pierre-Alain Carrupt; Claudia Simões-Pires; Alessandra Nurisso
Journal:  Sci Rep       Date:  2016-07-12       Impact factor: 4.379

Review 4.  Aurones: A Golden Resource for Active Compounds.

Authors:  Ilaria Mazziotti; Giovanni Petrarolo; Concettina La Motta
Journal:  Molecules       Date:  2021-12-21       Impact factor: 4.411

5.  Exploring the 2'-Hydroxy-Chalcone Framework for the Development of Dual Antioxidant and Soybean Lipoxygenase Inhibitory Agents.

Authors:  Ioanna Kostopoulou; Andromachi Tzani; Nestor-Ioannis Polyzos; Maria-Anna Karadendrou; Eftichia Kritsi; Eleni Pontiki; Thalia Liargkova; Dimitra Hadjipavlou-Litina; Panagiotis Zoumpoulakis; Anastasia Detsi
Journal:  Molecules       Date:  2021-05-08       Impact factor: 4.411
  5 in total

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