PLATINUM(II) COMPLEXES OF FUNCTIONALIZED MALONATO LIGANDS - UNEQUIVOCAL SYNTHESIS, INTERACTION WITH A TETRADEOXYRIBONUCLEOTIDE AND DEOXYRIBONUCLEIC-ACID

The unequivocal syntheses of four cis-PtL2{(O2C)2CH(CH2)nCO2H}! compl exes L2 = (NH3)2 or trans-cyclohexane-1,2-diamine, n = 1 or 4! has be en achieved, avoiding any interaction between the pendant carboxyl gro up and the platinum. The complexes have been characterized by elementa l analysis, C-13 NMR and FAB mass spectroscopy. Their interaction with a tetradeoxyribonucleotide d(T-G-G-T) (G = guanosine, T = ribosylthym ine) and DNA (in vitro) has been investigated to show that they form a dducts of the type PtL2{(GpG)-N7,N7'}! as do the known therapeuticall y active platinum complexes. However the presence of the free carboxyl function increases significantly the reactivity with respect to that of the related non-functionalized malonato complexes PtL2{H2C(CO2)2}! .