Synthesis, Biological Evaluations and DNA Interaction Studies on Trans Platinum(II) Thiolate Complexes

The serendipitous discovery of the cytotoxicity of cisplatin and its successful use in cancer therapy since the 1970s have led to an enormous amount of research in this area [1]. One major problem with cisplatin anticancer drug is the development of cell resistance, and thus, there is a continuing need for new and highly active cytotoxic platinum compounds. Some recent work has focused on the development of trans platinum complexes, which were initially neglected after it was reported that trans- [PtCl2(NH3)2] is not cytotoxic [2]. We have been interested in the preparation and applications of platinum complexes containing thiolate ligands [3]. As an extension of this work, we present here the preparation, characterization, and cytotoxicity studies of trans platinum(II) complexes containing allyldiphenylphosphane (PPh2Allyl) ligand as well as various thiolate ligands (Fig. 1). The cytotoxic activities of complexes have been evaluated against three human cancer cell lines: ovarian carcinoma (SKOV3), lung carcinoma (A549)and breast carcinoma (MCF‐7). Also, the induction of cellular apoptosis for complexes were studied on MCF‐7 cell line. Our results indicated that complexes could induce apoptosis in cancerous cells in a dose‐dependent manner.