Mutagenic activity of some platinum complexes: Chemical properties and biological activity†

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Abstract
In order to find correlations between chemical reactivity and biological activity, we have started an investigation on the mutagenic activity of different platinum‐chloroamine complexes towards different strains of Salmonella Typhimurium. The first class of compounds examined includes complexes of general formula cis‐[PtCl2(amine)(L)] in which L represents a strong trans‐labilizing ligand. Using dimethylsulphoxide as solvent these compounds were not toxic or mutagenic, on the contrary in acetone they were toxic towards all strains of bacteria independently from their excision‐repair ability. An entirely different behaviour was exhibited by a second class of compounds having general formula cis‐[PtCl2(amine)2] which includes also cis‐dichlorodi‐ammoniaplatinum(II) (cis‐DDP). These compounds were much less toxic than the previous ones in acetone and were mutagenic; moreover they were able to discriminate between different bacteria strains. Therefore some complexes were active only towards hisG46/pKM101 strain, others towards both hisG46/pKM101 and hisD3052/pKM101 bacteria. Furthermore some compounds (particularly those with H2N‐Bu t and H2NCHMePh), differently from cis‐DDP, were mutagenic only towards excision‐repair deficient strains indicating that they can cause only a specific and well reparable damage.