Synthesis, biological evaluation and molecular modeling studies of some novel thiazolidinediones with triazole ring
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 show...
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Veröffentlicht in: | European journal of medicinal chemistry 2013-12, Vol.70, p.308-314 |
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Hauptverfasser: | , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | 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.
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•Several thiazolidiendiones tagged with 1,2,3-triazoles were synthesized.•Compounds 3d, 3e and 3j showed significant α-glucosidase inhibition activity.•The cytotoxic activity of compounds was assessed using MTT reduction assay.•Docking results of 3d, 3e and 3j with α-glucosidase were comparable with Acarbose. |
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ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/j.ejmech.2013.10.005 |