Design, Synthesis, and Evaluation of 3-Aryl-4-pyrrolyl-maleimides as Glycogen Synthase Kinase-3β Inhibitors

被引：6

作者：

Ye, Qing ^{[1
]}

Li, Meng ^{[1
]}

Zhou, Yu-Bo ^{[2
]}

Cao, Jia-Yu ^{[2
]}

Xu, Lei ^{[2
]}

Li, Yu-Jin ^{[1
]}

Han, Liang ^{[1
]}

Gao, Jian-Rong ^{[1
]}

Hu, Yong-Zhou ^{[3
]}

Li, Jia ^{[2
]}

机构：

[1] Zhejiang Univ Technol, State Key Lab Breeding Base Green Chem Synth Tech, Hangzhou 310032, Zhejiang, Peoples R China

[2] Zhejiang Univ, Coll Pharmaceut Sci, ZJU ENS Joint Lab Med Chem, Hangzhou 310003, Zhejiang, Peoples R China

[3] Natl Ctr Drug Screening, Shanghai, Peoples R China

来源：

ARCHIV DER PHARMAZIE | 2013年 / 346卷 / 05期

关键词：

3-Aryl-4-pyrrolyl-maleimides; Cellular activity; Enzymatic activity; GSK-3; inhibitors; PROTEIN-KINASE; ALZHEIMERS-DISEASE; 1,2,4-TRIAZOLE DERIVATIVES; TAU-PHOSPHORYLATION; FUNGICIDAL ACTIVITY; POTENT INHIBITORS; CRYSTAL-STRUCTURE; BETA; BISINDOLYLMALEIMIDES; GSK-3;

D O I：

10.1002/ardp.201300008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-aryl-4-pyrrolyl-maleimides were designed, synthesized, and evaluated for their glycogen synthase kinase-3 (GSK-3) inhibitory activity. Most compounds exhibited potent activity against GSK-3. Among them, compounds 11a, 11c, 11h, 11i, and 11j significantly reduced A-induced Tau hyperphosphorylation, showing the inhibition of GSK-3 at the cellular level. Structureactivity relationships were discussed based on the experimental data obtained.

引用

页码：349 / 358

页数：10

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