Non-ATP competitive glycogen synthase kinase 3β (GSK-3β) inhibitors: Study of structural requirements for thiadiazolidinone derivatives
作者： Ana Castro , Arantxa Encinas , Carmen Gil , Stefan Bräse , Williams Porcal
DOI: 10.1016/J.BMC.2007.09.016
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摘要: Abstract The 2,4-disubstituted thiadiazolidinones (TDZD) were described as the first non-ATP competitive GSK-3β inhibitors. New modifications in this heterocyclic ring are here reported to study influence on biological activity. basic skeleton of 1,2,4-thiadiazole and also one carbonyl groups kept, while different introduced positions 3 5, respectively. activity new thiadiazole derivatives synthesized showed IC 50 values for some compounds micromolar range. Additionally, ATP competition studies have been carried out, showing that well generation TDZD, these act a non-competitive manner. With study, additional requirements TDZD family delineated.
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