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

Lorena Giovagnini, Luca Ronconi, Donatella Aldinucci, Debora Lorenzon, Sergio Sitran, Dolores Fregona

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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, 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 IC 50 values slightly higher than those recorded for cisplatin; moreover, [Au(MSDT)X2] 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)X2] complexes induces apoptosis, as determined by an Apo2.7 assay.

Original languageEnglish
Pages (from-to)1588-1595
Number of pages8
JournalJournal of Medicinal Chemistry
Volume48
Issue number5
DOIs
Publication statusPublished - Mar 10 2005

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Palladium
Cytotoxicity
Platinum
HeLa Cells
Gold
Antineoplastic Agents
Cisplatin
Cells
Apoptosis
Cell Line
HL-60 Cells
Growth
Bioactivity
Assays
Esters
Adenocarcinoma
Derivatives
Pharmaceutical Preparations
In Vitro Techniques
Inhibition (Psychology)

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Synthesis, characterization, and comparative in vitro cytotoxicity studies of platinum(II), palladium(II), and gold(III) methylsarcosinedithiocarbamate complexes. / Giovagnini, Lorena; Ronconi, Luca; Aldinucci, Donatella; Lorenzon, Debora; Sitran, Sergio; Fregona, Dolores.

In: Journal of Medicinal Chemistry, Vol. 48, No. 5, 10.03.2005, p. 1588-1595.

Research output: Contribution to journalArticle

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