257874-86-5Relevant articles and documents
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3β (GSK-3β) inhibitors
Ye, Qing,Xu, Guiqing,Lv, Dan,Cheng, Zhe,Li, Jia,Hu, Yongzhou
experimental part, p. 4302 - 4312 (2009/10/10)
A series of novel 4-azaindolyl-indolyl-maleimides were synthesized and evaluated for their GSK-3β inhibitory activity. Most compounds exhibited high potency to GSK-3β. Among them, compound 7c was the most promising GSK-3β inhibitor. Preliminary structure-activity relationships were discussed based on the experimental data obtained and showed that different substituents on the indole ring and side chains at 1-position of indole had varying degrees of influence on the GSK-3β inhibitory potency. In a cell-based functional assay, compounds 7c and 15a significantly reduced Aβ-induced Tau hyperphosphorylation by inhibiting GSK-3β.
Synthesis of anilino-monoindolylmaleimides as potent and selective PKCβ inhibitors
Tanaka, Masahiro,Sagawa, Shoichi,Hoshi, Jun-Ichi,Shimoma, Fumito,Matsuda, Isamu,Sakoda, Kenji,Sasase, Tomohiko,Shindo, Masanori,Inaba, Takashi
, p. 5171 - 5174 (2007/10/03)
The synthesis and enzyme inhibitory activity of PKCIβ-selective inhibitors possessing the novel pharmacophore of anilino-monoindolylmaleimide are described.
KINASE INHIBITORS
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Page/Page column 40, (2010/02/07)
The present invention provides kinase inhibitors of Formula (I)
DISUBSTITUTED MALEIMIDE COMPOUNDS AND MEDICINAL UTILIZATION THEREOF
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, (2008/06/13)
The present invention relates to a disubstituted maleimide compound of the formula [I] wherein R1 is hydrogen or alkyl, R2 is aryl, cycloalkyl or heterocyclic group, R3, R5, R6, R7 and Rsu