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Design, Synthesis, and Evaluation of 3‐Aryl‐4‐pyrrolyl‐maleimides as Glycogen Synthase Kinase‐3β Inhibitors
Author(s) -
Ye Qing,
Li Meng,
Zhou YuBo,
Cao JiaYu,
Xu Lei,
Li YuJin,
Han Liang,
Gao JianRong,
Hu YongZhou,
Li Jia
Publication year - 2013
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201300008
Subject(s) - gsk 3 , glycogen synthase , chemistry , hyperphosphorylation , aryl , gsk3b , kinase , enzyme , structure–activity relationship , atp synthase , biochemistry , stereochemistry , in vitro , organic chemistry , alkyl
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 11a , 11c , 11h , 11i , and 11j 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.