Adelaide Research & Scholarship
Please use this identifier to cite or link to this item:
https://hdl.handle.net/2440/118656
| Citations | ||
| Scopus | Web of Science® | Altmetric |
|---|---|---|
|
?
|
?
|
|
| Type: | Journal article |
| Title: | Aurones as histone deacetylase inhibitors: identification of key features |
| Author: | Zwick, V. Chatzivasileiou, A.-O. Deschamps, N. Roussaki, M. Simões-Pires, C.A. Nurisso, A. Denis, I. Blanquart, C. Martinet, N. Carrupt, P.-A. Detsi, A. Cuendet, M. |
| Citation: | Bioorganic and Medicinal Chemistry Letters, 2014; 24(23):5497-5501 |
| Publisher: | Elsevier |
| Issue Date: | 2014 |
| ISSN: | 0960-894X 1464-3405 |
| Statement of Responsibility: | Vincent Zwick, Alkiviadis-Orfefs Chatzivasileiou, Nathalie Deschamps, Marina Roussaki, Claudia A. Simões-Pires ... Iza Denis ... et al. |
| 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: | Histone deacetylase; structure activity relationship; docking; aurone |
| Rights: | © 2014 Elsevier Ltd. All rights reserved. |
| DOI: | 10.1016/j.bmcl.2014.10.019 |
| Published version: | http://dx.doi.org/10.1016/j.bmcl.2014.10.019 |
| Appears in Collections: | Aurora harvest 4 Medicine publications |
Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.