Design, Synthesis, and Evaluation of 3‐Aryl‐4‐pyrrolyl‐maleimides as Glycogen Synthase Kinase‐3β Inhibitors. Issue 5 (15th April 2013)

• Record Type: Journal Article
• Authors: Ye, Qing; Li, Meng; Zhou, Yu‐Bo; Cao, Jia‐Yu; Xu, Lei; Li, Yu‐Jin; Han, Liang; Gao, Jian‐Rong; Hu, Yong‐Zhou; Li, Jia
• Is Part Of: Archiv der Pharmazie. Volume 346:Issue 5(2013:May)
• Page Start: 349
• Page End: 358
• Publication Date: 2013-04-15
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201300008
• Languages: English
• ISSNs: 0365-6233

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>A series of 3‐aryl‐4‐pyrrolyl‐maleimides were designed, synthesized, and evaluated for their glycogen synthase kinase‐3β (GSK‐3β) inhibitory activity. Most compounds exhibited potent activity against GSK‐3β. Among them, compounds <bold>11a</bold>, <bold>11c</bold>, <bold>11h</bold>, <bold>11i</bold>, and <bold>11j</bold> significantly reduced Aβ‐induced Tau hyperphosphorylation, showing the inhibition of GSK‐3β at the cellular level. Structure–activity relationships were discussed based on the experimental data obtained.</p> </abstract>