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Issue 43, 2018
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Synthesis, chemical characterization and cancer cell growth-inhibitory activities of Cu(II) and Ru(III) aliphatic and aromatic dithiocarbamato complexes

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Abstract

In this paper, we focused on the analysis of the effects mediated by different cyclic dithiocarbamic ligands (DTC) on three classes of antiproliferative coordination compounds, namely, Ru(III) complexes with the general formulae [Ru(DTC)3] and [Ru2(DTC)5]Cl, and the neutral Cu(II) derivatives of the type [Cu(DTC)2]. In particular, we present the synthesis and characterization of a library of total 23 coordination compounds containing Ru(III) or Cu(II) as the biologically-active metal center and two or more dithiocarbamato (DTC) ligands derived from cyclic amines (aliphatic or aromatic). Several techniques including elemental analysis, X-ray crystallography, ESI-MS, 1H-NMR spectroscopy, FT-IR and UV-Vis spectrophotometry were used to characterize the compounds, which highlighted the different electronic behaviors generated by the substituents within the DTC moiety. Moreover, the synthesized compounds were tested for their stability in order to investigate their antiproliferative activity against 3 human cancer cell lines, namely, HeLa, HepG2 and HepG2/SB3. In particular, HepG2/SB3 was chosen for its aggressiveness due to upregulation of the anti-apoptotic protein SerpinB3. Finally, the most promising compounds are studied in terms of log P. Overall, the results reveal the drug-likeness of some of the derivatives of copper(II) and ruthenium(III).

Graphical abstract: Synthesis, chemical characterization and cancer cell growth-inhibitory activities of Cu(ii) and Ru(iii) aliphatic and aromatic dithiocarbamato complexes

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Publication details

The article was received on 20 Jul 2018, accepted on 29 Sep 2018 and first published on 04 Oct 2018


Article type: Paper
DOI: 10.1039/C8DT02965B
Citation: Dalton Trans., 2018,47, 15477-15486
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    Synthesis, chemical characterization and cancer cell growth-inhibitory activities of Cu(II) and Ru(III) aliphatic and aromatic dithiocarbamato complexes

    L. Brustolin, C. Nardon, N. Pettenuzzo, N. Zuin Fantoni, S. Quarta, F. Chiara, A. Gambalunga, A. Trevisan, L. Marchiò, P. Pontisso and D. Fregona, Dalton Trans., 2018, 47, 15477
    DOI: 10.1039/C8DT02965B

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