200711-88-2Relevant academic research and scientific papers
Isoindole-1,3-dione derivatives as RSK2 inhibitors: Synthesis, molecular docking simulation and SAR analysis
Zhou, Wei,Li, Shiliang,Lu, Weiqiang,Yuan, Jun,Xu, Yufang,Li, Honglin,Huang, Jin,Zhao, Zhenjiang
, p. 292 - 296 (2016)
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.
