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Eur J Med Chem ; 70: 308-14, 2013.
Article in English | MEDLINE | ID: mdl-24177357

ABSTRACT

A new series of thiazolidinedione derivatives were synthesized and evaluated for in vitro α-glucosidase inhibition and anticancer activities. Compounds 3d, 3e and 3j showed potential α-glucosidase inhibition with IC50 values ranging between 0.1 and 0.3 µg/ml whereas compounds 3i, 3j and 3k have showed better anticancer activity towards human cancer cell lines IMR-32 (neuroblastoma), Hep-G2 (hepatoma) and MCF-7 (breast). Molecular docking studies revealed compounds 3d, 3e and 3j are potent inhibitors of α-glucosidase and also showed compliance with standard parameters of drug likeness.


Subject(s)
Antineoplastic Agents/pharmacology , Enzyme Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors , Thiazolidinediones/pharmacology , Triazoles/chemistry , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Hep G2 Cells , Humans , MCF-7 Cells , Models, Molecular , Molecular Structure , Structure-Activity Relationship , Thiazolidinediones/chemical synthesis , Thiazolidinediones/chemistry , alpha-Glucosidases/metabolism
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