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Investigation of the cytotoxic potential of methyl imidazole-derived thiosemicarbazones and theircopper(II) complexes with dichloroacetate as co-ligand

Abstract

A series of six imidazole-derived thiosemicarbazones (HL1‒HL6) and their copper(II) complexes (1‒6) were synthesised and characterised by analytical, spectroscopic, electrochemical and single crystal X-ray diffraction techniques. In addition, solution studies and the results of antiproliferative activity in human cancer cell lines with some insights into the mechanism of cancer cell death are also reported. In particular, the substitution of one hydrogen at terminal N-atom of thiosemicarbazide moiety by phenyl group induced slightly enhanced cell inhibition growth potency of proligands HL3 and HL6 compared to other investigated proligands in all cancer cell lines, while their copper(II) complexes 3 and 6 exhibit 2.4- and 4.7-fold increase of activity compared to parent proligands in A549 cancer cell line, respectively. The complex formation of the proligands with copper(II) increased their antiproliferative activity in all investigated cell lines. The cell cycle perturbations, apoptotic potential and the analysis of morphological changes in A549 cell line induced by 3 and 6 revealed rather cytostatic than cytotoxic effect.

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Publication details

The article was received on 09 Aug 2018, accepted on 09 Nov 2018 and first published on 09 Nov 2018


Article type: Paper
DOI: 10.1039/C8NJ04041A
Citation: New J. Chem., 2018, Accepted Manuscript
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    Investigation of the cytotoxic potential of methyl imidazole-derived thiosemicarbazones and theircopper(II) complexes with dichloroacetate as co-ligand

    O. Palamarciuc, M. N.M. Milunović, A. Sirbu, E. Stratulat, A. Pui, N. Gligorijević, S. Radulović, J. Kozisek, D. Darvasiova, P. Rapta, E. A. Enyedy, G. Novitchi, S. Sova and V. Arion, New J. Chem., 2018, Accepted Manuscript , DOI: 10.1039/C8NJ04041A

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