SYNTHESIS AND BIOLOGICAL-ACTIVITY OF GOLD AND TIN-COMPOUNDS IN OVARIAN-CANCER CELLS

We have investigated the patterns of in vitro cytotoxicity, induced by six newly synthesized gold and tin compounds, in three human ovarian cancer cell lines (SW 626, IGROV 1 and OVCAR-3). Four gold compounds, i.e. gold(I)lupinylsulfide hydrochloride [1] (containing a naked gold atom), triethylphosphinogold(I)lupinylsulfide hydrochloride [2], triph enyl-phosphinogold(I)lupinylsulfide hydrochloride [3] and 1,2-bis(diph enylphosphino)ethane bis[gold(I)lupinylsulfide] dihydrochloride [4] (a ll containing a gold atom coordinated with different phosphines), were prepared. Moreover, the iethylphosphinogold(I)(2-diethylamino)ethylsu lfide hydrochloride [5] in which the simple diethylaminoethylthiol rep laced the bulky lupinylthiol was synthesized. The tin compound, trieth yltin(IV)lupinylsulfide hydrochloride [6], was also studied. Comparati ve tests with cisplatin, the most widely used antitumor agent in ovari an cancer, were carried out in biological investigations. In vitro cyt otoxicity, by MTT assay, showed that compound [4] and compound [6] exh ibited interesting antiproliferative activity in all the three cell li nes (mean IC50=1.3 and 0.7 mu M, respectively) compared to cisplatin ( mean IC50=4.8 mu M). In addition, the PA-1 cell line, more sensitive t o cisplatin (IC50=0.6 mu M), was included as a comparison in the study . Cell count assays confirmed the cytotoxic properties of compounds [4 ] and [6] against the four cell lines, reporting higher growth inhibit ion potency than cisplatin, with IC50 values in the sub micromolar ran ge. [(C) 1998 Lippincott Williams & Wilkins.].