On January 31, 2020, Francisco, Carla S.; Javarini, Clara L.; Barcelos, Iatahanderson de S.; Morais, Pedro A. B.; de Paula, Heberth; Borges, Warley de S.; Cunha Neto, Alvaro; Lacerda, Valdemar published an article.SDS of cas: 621-37-4 The title of the article was Synthesis of Coumarin Derivatives as Versatile Scaffolds for GSK-3β Enzyme Inhibition. And the article contained the following:
Glycogen synthase kinase-3 (GSK-3) is involved in the phosphorylation and inactivation of glycogen synthase. GSK-3 inhibitors have been associated with a variety of diseases, including Alzheimer’s disease (AD), diabetes type II, neurol. disorders, and cancer. The inhibition of GSK-3β isoforms is likely to represent an effective strategy against AD. The present work aimed to design and synthesize coumarin derivatives to explore their potential as GSK-3β kinase inhibitors. The through different synthetic methods were used to prepare coumarin derivatives The GSK-3β activity was measured through the ADP-GloTM Kinase Assay, which quantifies the kinasedependent enzymic production of ADP from ATP, using a coupled-luminescence-based reaction. A docking study was performed by using the crystallog. structure of the staurosporine/GSK-3β complex [Protein Data Bank (PDB) code: 1Q3D]. The eleven coumarin derivatives were obtained and evaluated as potential GSK-3β inhibitors. Addnl., in silico studies were performed. The results revealed that the compounds 5c, 5d, and 6b inhibited GSK-3β enzymic activity by 38.97-49.62% at 1 mM. The other coumarin derivatives were tested at 1 mM, 1μM, and 1 nM concentrations and were shown to be inhibitor candidates, with significant IC50 (1.224-6.875μM) values, except for compound 7c (IC50 = 10.809μM). Docking simulations showed polar interactions between compound 5b and Lys85 and Ser203, clarifying the mechanism of the most potent activity. The coumarin derivatives 3a and 5b, developed in this study, showed remarkable activity as GSK-3β inhibitors. The experimental process involved the reaction of 3-Hydroxyphenylacetic acid(cas: 621-37-4).SDS of cas: 621-37-4
The Article related to methoxyphenylcoumarin gsk3beta inhibitor alzheimer disease antialzheimer agent, biological activity, coumarin, coumarin derivatives, enzymatic inhibition, gsk-3β, molecular docking. and other aspects.SDS of cas: 621-37-4
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts