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- W3047277584 endingPage "20186" @default.
- W3047277584 startingPage "20170" @default.
- W3047277584 abstract "A series of novel anticancer hydrazinotriazolothiadiazine-based derivatives were designed based on the structure–activity relationship of the previously reported anticancer triazolothiadiazines. These derivatives were synthesized and biologically screened against full NCI-60 cancer cell lines revealing compound 5l with a potential antiproliferative effect. 5l was screened over 16 kinases to study its cytotoxic mechanism which showed to inhibit glycogen synthase kinase-3 β (GSK-3β) with IC50 equal to 0.883 μM and 14-fold selectivity over CDK2. Also, 5l increased active caspase-3 levels, induced cell cycle arrest at the G2-M phase, and increased the percentage of Annexin V-fluorescein isothiocyanate-positive apoptotic cells in PC-3 prostate cancer-treated cells. Molecular docking and dynamics were performed to predict the binding mode of 5l in the GSK-3β ATP binding site. 5l can be utilized as a starting scaffold for developing potential GSK-3β inhibitors." @default.
- W3047277584 created "2020-08-10" @default.
- W3047277584 creator A5003776521 @default.
- W3047277584 creator A5007843479 @default.
- W3047277584 creator A5032282292 @default.
- W3047277584 creator A5079571280 @default.
- W3047277584 date "2020-08-06" @default.
- W3047277584 modified "2023-10-12" @default.
- W3047277584 title "Design, Synthesis, and Biological Evaluation of Novel 7<i>H</i>-[1,2,4]Triazolo[3,4-<i>b</i>][1,3,4]thiadiazine Inhibitors as Antitumor Agents" @default.
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