4814-15-7Relevant academic research and scientific papers
Synthesis of aryl anilinomaleimide based derivatives as glycogen synthase kinase-3β inhibitors with potential role as antidepressant agents
Tantray, Mushtaq A.,Khan, Imran,Hamid, Hinna,Alam, Mohammad Sarwar,Dhulap, Abhijeet,Kalam, Abul
, p. 6109 - 6119 (2016/07/16)
A series of aryl anilinomaleimide based derivatives has been synthesized and evaluated for in vitro glycogen synthase kinase-3β (GSK-3β) inhibitory activity. A large number of compounds from the series exhibited moderate to potent inhibitory activity against GSK-3β, with more than one-third of the compounds showing inhibition with IC50 values 50 values of 0.09, 0.12, 0.17, 0.19, 0.21 and 0.23 μM respectively), were further investigated for antidepressant activity by the widely accepted forced swim test and tail suspension test (FST and TST) models. All the tested compounds displayed antidepressant-like effects, particularly compounds 8j and 8b, which exhibited significant antidepressant activity, about 1.4-fold higher than fluoxetine, a standard antidepressant drug in both FST and TST. Preliminary structure-activity relationships have also been generated based on the experimental data obtained.
Synthesis, cytotoxicity and protein kinase C inhibition of arylpyrrolylmaleimides
Xu, Gui-Qing,Zhang, Chong,Zhang, Lei,Zhou, Xing-Lu,Yang, Bo,He, Qiao-Jun,Hu, Yong-Zhou
experimental part, p. 273 - 280 (2009/04/04)
A series of novel arylpyrrolylmaleimides was synthesized and evaluated for their in-vitro cytotoxicity against various human cancer cell lines and their protein-kinase C inhibitory activity. Some of the compounds showed high or moderate cytotoxic activity
3-Anilino-4-arylmaleimides: Potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3)
Smith, David G.,Buffet, Marianne,Fenwick, Ashley E.,Haigh, David,Ife, Robert J.,Saunders, Martin,Slingsby, Brian P.,Stacey, Rachel,Ward, Robert W.
, p. 635 - 639 (2007/10/03)
Potent 3-anilino-4-arylmaleimide glycogen synthase kinase-3 (GSK-3) inhibitors have been prepared using automated array methodology. A number of these are highly selective, having little inhibitory potency against more than 20 other protein kinases.
