Synthesis, characterization, and comparative in vitro cytotoxicity studies of platinum(II), palladium(II), and gold(III) methylsarcosinedithiocarbamate complexes

被引:164
作者
Giovagnini, L
Ronconi, L
Aldinucci, D
Lorenzon, D
Sitran, S
Fregona, D
机构
[1] Univ Padua, Dept Chem Sci, I-35131 Padua, Italy
[2] IRCCS, CRO Res Area, Clin & Expt Hematol Res Unit, I-33081 Aviano, PN, Italy
[3] CNR Res Area, Inst Inorgan & Surfaces Chem, I-35127 Padua, Italy
关键词
D O I
10.1021/jm049191x
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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, 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 has been compared to the well-known platinum-based anticancer agent cisplatin. On the basis of these experimental results, [Pd-(MSDT)X](n) (MSDT = methylsarcosinedithiocarbamate; X = Cl, Br) complexes show a strong dose-dependent growth inhibition of both HL60 and HeLa cells, with IC50 values slightly higher than those recorded for cisplatin; moreover, [Au(MSDT)X-2] activity appears significantly higher or, at least, comparable to that of the reference drug. Exposure of both cell lines to [Pd(MSDT)X](n) and [Au(MSDT)X-2] complexes induces apoptosis, as determined by an Apo2.7 assay.
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页码:1588 / 1595
页数:8
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