Synthesis and biological evaluation of 3-substituted 2-oxindole derivatives as new glycogen synthase kinase 3β inhibitors

Add time:07/11/2019    Source:sciencedirect.com

Glycogen synthase kinase 3β (GSK-3β) is a widely investigated molecular target for numerous diseases including Alzheimer’s disease, cancer, and diabetes mellitus. Inhibition of GSK-3β activity has become an attractive approach for treatment of diabetes and cancer. We report the discovery of novel GSK-3β inhibitors of 3-arylidene-2-oxindole scaffold with promising activity. The most potent compound 3a inhibits GSK-3β with IC50 4.19 nM. In a cell-based assay 3a shows no significant leucocyte toxicity at 10 µM and is moderately cytotoxic against A549 cells. Compound 3a demonstrated high antidiabetic efficacy in obese streptozotocin-treated rats improving glucose tolerance at a dose of 50 mg/kg body weight thus representing an interesting lead for further optimization.

We also recommend Trading Suppliers and Manufacturers of N'-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-1,3-benzodioxole-5-carbohydrazide (cas 342000-80-0). Pls Click Website Link as below: cas 342000-80-0 suppliers

Prev:Fusaric acid and analogues as Gram-negative bacterial quorum sensing inhibitors
Next:Synthesis, spectroscopy characterization and biological activities of some novel 1-(3-(N,N-dimethylamino)-1-(5-substituted thiophene-2-yl) propylidene semicarbazone Mannich base derivatives)