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 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 characterized 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).

Zinc(II) Complexes with Dithiocarbamato Derivatives: Structural Characterization and Biological Assays on Cancerous Cell Lines

NAGY, ESTER;MONTOPOLI, MONICA;CAPARROTTA, LAURA;FREGONA, DOLORES
2012

Abstract

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 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 characterized 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).
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11577/2511190
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