Jump to main content
Jump to site search

Issue 2, 2016
Previous Article Next Article

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

Author affiliations

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

Back to tab navigation

Supplementary files

Publication details

The article was received on 14 Oct 2015, accepted on 19 Nov 2015 and first published on 25 Nov 2015


Article type: Research Article
DOI: 10.1039/C5MD00469A
Author version
available:
Download author version (PDF)
Med. Chem. Commun., 2016,7, 292-296

  •   Request permissions

    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

Search articles by author

Spotlight

Advertisements