This work reports on the synthesis, characterization and biological activity of new coordination compounds of the type [M(TSDTM)X2] (M=Pt(II), Pd(II); X=Cl, Br; TSDTM=ter-butylsarcosine(S-methyl)dithiocarbamate) and [Pd(TSDT)X]n (TSDT=ter-butylsarcosinedithiocarbamate) in order to study their behavior as potential antitumor agents. All the synthesized compounds were characterized by means of elemental analysis, FT-IR, 1H and 13C-NMR spectroscopy and thermogravimetric analysis, suggesting a chelate S,S′ structure of the TSDTM/TSDT ligand in a square-planar geometry. Finally, the synthesized complexes have been tested for in vitro cytotoxic activity against human leukemic HL60 and adenocarcinoma HeLa cells; the most active compound [Pt(TSDTM)Br2], characterized by IC50 values very similar to those of the reference compound (cisplatin), was also tested for in vitro nephrotoxicity showing a very low renal cytotoxicity as compared to cisplatin itself.
Pt(II) and Pd(II) derivatives of ter-butlsarcosinedithiocarbamate. Synthesis, chemical, and biological characterization and in vitro nephrotoxicity
FREGONA, DOLORES;GIOVAGNINI, LORENA;RONCONI, LUCA;MARZANO, CRISTINA;TREVISAN, ANDREA;
2003
Abstract
This work reports on the synthesis, characterization and biological activity of new coordination compounds of the type [M(TSDTM)X2] (M=Pt(II), Pd(II); X=Cl, Br; TSDTM=ter-butylsarcosine(S-methyl)dithiocarbamate) and [Pd(TSDT)X]n (TSDT=ter-butylsarcosinedithiocarbamate) in order to study their behavior as potential antitumor agents. All the synthesized compounds were characterized by means of elemental analysis, FT-IR, 1H and 13C-NMR spectroscopy and thermogravimetric analysis, suggesting a chelate S,S′ structure of the TSDTM/TSDT ligand in a square-planar geometry. Finally, the synthesized complexes have been tested for in vitro cytotoxic activity against human leukemic HL60 and adenocarcinoma HeLa cells; the most active compound [Pt(TSDTM)Br2], characterized by IC50 values very similar to those of the reference compound (cisplatin), was also tested for in vitro nephrotoxicity showing a very low renal cytotoxicity as compared to cisplatin itself.Pubblicazioni consigliate
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