Zinc(II) complexes with dithiocarbamato derivatives: Structural characterisation and biological assays on cancerous cell lines

Zinc is one of the most important trace elements in the body and it is essential as a cofactor for the structure and function of a number of cellular molecules including enzymes, transcription factors, cellular signalling proteins and DNA repair enzymes. On the other hand, recent studies have shown that zinc could play a role both in the development of various cancers and in the induction of apoptosis in some cell types, however, no established common relationships of zinc with cancer development and progression have been identified. To date, in our research group different metal-dithiocarbamato complexes have been designed that were expected to resemble the main features of cisplatin together with higher activity, improved selectivity and bioavailability, and lower side-effects. On the basis of the obtained encouraging achievements with other metals (such as gold and copper) we have decided to enlarge the studies to the complexes of zinc(II) using the same ligands. Hereby, we report the results on the synthesis and characterisation of ZnL2 complexes with five different dithiocarbamato derivatives, such as dimethyl-(DMDT), pyrrolidine-(PyDT), methyl-(MSDT), ethyl-(ESDT) and tert-butyl-(TSDT) sarcosinedithiocarbamate. All the obtained compounds have fully been characterised by means of several spectroscopic techniques. In addition, the crystal structure of [Zn(MSDT)2]2 dinuclear complex is also reported. In order to evaluate the in vitro cytotoxic properties, some biological assays have been carried out on a panel of human tumour cell lines sensible and resistant to cisplatin. Some of the tested compounds show cytotoxicity levels comparable or even greater than the reference drug (cisplatin).

Hereby, we report the results on the synthesis, characterisation and in vitro cytotoxic activity assays of new bis(dithiocarbamato)zinc(II) complexes derived from methyl-, ethyl and tert-buthylsarcosine ester. Some of the metal complexes have cytotoxicity levels comparable or even greater than the reference drug (cisplatin) on numerous human tumour cell lines.Figure optionsDownload as PowerPoint slideHighlights
► Novel zinc(II) dithiocarbamato complexes have been synthetized and characterised.
► X-ray structure of the [Zn(MSDT)2]2 dimeric complex was determined.
► Some compounds show interesting cytotoxic activity on numerous tumour cell lines.
► The anticancer activity is associated with cell cycle arrest and apoptosis.