This work reports on the synthesis, characterization and in vitro cytotoxic activity of some new platinum(II), palladium(II) and gold(III) derivatives of methylsarcosinedithiocarbamate and its S-methyl ester, in order to study their behavior as potential antitumor agents. The biological activity of these compounds, as determined by growth inhibition and apoptosis induction, has been investigated in both human leukemic promyelocites HL60 and human squamous cervical adenocarcinoma HeLa cell lines, and their activity compared to the well known platinum-based anticancer agent cisplatin. On the basis of these experimental results, ËPd(MSDT)XÍn (MSDT = methylsarcosinedithiocarbamate; X = Cl, Br) complexes determine a strong dose-dependent growth inhibition of both HL60 and HeLa cells, with IC50 values slightly higher than those recorded for cisplatin; moreover, ËAu(MSDT)X2] activity appears significantly higher or, at least, comparable to that of the reference drug. Exposure of both cell lines to ËPd(MSDT)XÍn and ËAu(MSDT)X2] complexes induces apoptosis, as determined by Apo2.7 assay.
Synthesis, Characterization and Comparative In Vitro Cytotoxicity Studies of Platinum(II), Palladium(II) and Gold(III) Methylsarcosinedithiocarbamate Complexes
Sitran S;
2005
Abstract
This work reports on the synthesis, characterization and in vitro cytotoxic activity of some new platinum(II), palladium(II) and gold(III) derivatives of methylsarcosinedithiocarbamate and its S-methyl ester, in order to study their behavior as potential antitumor agents. The biological activity of these compounds, as determined by growth inhibition and apoptosis induction, has been investigated in both human leukemic promyelocites HL60 and human squamous cervical adenocarcinoma HeLa cell lines, and their activity compared to the well known platinum-based anticancer agent cisplatin. On the basis of these experimental results, ËPd(MSDT)XÍn (MSDT = methylsarcosinedithiocarbamate; X = Cl, Br) complexes determine a strong dose-dependent growth inhibition of both HL60 and HeLa cells, with IC50 values slightly higher than those recorded for cisplatin; moreover, ËAu(MSDT)X2] activity appears significantly higher or, at least, comparable to that of the reference drug. Exposure of both cell lines to ËPd(MSDT)XÍn and ËAu(MSDT)X2] complexes induces apoptosis, as determined by Apo2.7 assay.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
