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Solution behaviour and biological activity of bisamidine complexes of platinum(II) (Articolo in rivista)

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Solution behaviour and biological activity of bisamidine complexes of platinum(II) (Articolo in rivista) (literal)

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C. Marzano; S. Mazzega Sbovata; F. Bettio; R.A. Michelin; R. Seraglia; T. Kiss; A. Venzo; R. Bertani (2007)
Solution behaviour and biological activity of bisamidine complexes of platinum(II)
in JBIC. Journal of biological inorganic chemistry (Print); Springer-Verlag, Berlin (Germania)
(literal)

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C. Marzano; S. Mazzega Sbovata; F. Bettio; R.A. Michelin; R. Seraglia; T. Kiss; A. Venzo; R. Bertani (literal)

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1,3 : Department of Pharmaceutical Sciences, University of Padova, Via F. Marzolo 5, 35131 Padua, Italy / 2,4,7 : Department of Chemical Processes of Engineering, University of Padova, Via F. Marzolo 9, 35131 Padua, Italy / 3,5,7 : CNR-ISTM. Institute of Sciences and Molecular Technologies, Via F. Marzolo 1, 35131 Padua, Italy / 6 : Department of Inorganic and Analytical Chemistry, University of Szeged, P.O. Box 440, 6701 Szeged, Hungary (literal)

Titolo

Solution behaviour and biological activity of bisamidine complexes of platinum(II) (literal)

Abstract

A series of platinum(II) amidine complexes were previously prepared with the aim of obtaining a new class of platinum-based antitumour drugs. This series includes compounds of the type cis-[PtCl2{Z-HN=C(NHMe)Me}2] and trans-[PtCl2{Z-HN=C(NHMe)Me}2] (1, 2 ), cis-[PtCl2{E-HN=C(NMe2)Me}2] and trans-[PtCl2{E-HN=C(NMe2)Me}2] (3 , 4), cis-[PtCl2{Z-HN=C(NHMe)Ph}2] and trans-[PtCl2{Z-HN=C(NHMe)Ph}2] (5 , 6), and cis-[PtCl2{HN=C(NMe2)Ph}2] and trans-[PtCl2{HN=C(NMe2)Ph}2] (7 , 8 ). The reactions with dimethyl sulfoxide were studied for complexes 5 - 8 ; the formation of cationic species con-taining coordinated dimethyl sulfoxide was demon-strated by NMR experiments and electrospray ionization mass spectrometry. In this work, the ami-dine platinum(II) complexes were tested for their in vitro cytotoxicity on a panel of various human cancer cell lines. The results indicate that the benzamidine complex 8 was the most effective derivative also cir-cumventing acquired cisplatin resistance as demon-strated by chemosensitivity tests performed on cisplatin-sensitive and cisplatin-resistant cell lines. The studies concerning the cellular DNA damage on both parental chemosensitive and resistant sublines suggest for the new trans-amidine complex a different mecha-nism of action compared with that exhibited by cis-platin. (literal)

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