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Issue 2, 2016
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Isoindole-1,3-dione derivatives as RSK2 inhibitors: synthesis, molecular docking simulation and SAR analysis

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Abstract

RSK2 (p90 ribosomal S6 kinase 2) is a serine/threonine kinase expressed in a variety of cancers. Molecular-targeted inhibition of RSK2 as a potential therapeutic strategy for human cancers has been documented. In this work, a series of isoindole-1,3-dione derivatives as novel RSK2 inhibitors were designed and synthesized from a hit discovered in our previous study. Some compounds were confirmed to be moderately potent RSK2 inhibitors with IC50 values of about 0.5 μM. Structure–activity relationship analysis and binding mode studies by molecular docking were performed.

Graphical abstract: Isoindole-1,3-dione derivatives as RSK2 inhibitors: synthesis, molecular docking simulation and SAR analysis

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Supplementary files

Article information


Submitted
14 Oct 2015
Accepted
19 Nov 2015
First published
25 Nov 2015

Med. Chem. Commun., 2016,7, 292-296
Article type
Research Article
Author version available

Isoindole-1,3-dione derivatives as RSK2 inhibitors: synthesis, molecular docking simulation and SAR analysis

W. Zhou, S. Li, W. Lu, J. Yuan, Y. Xu, H. Li, J. Huang and Z. Zhao, Med. Chem. Commun., 2016, 7, 292
DOI: 10.1039/C5MD00469A

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