Reactivity and Biological Properties of a Series of Cytotoxic PtI2(amine)(2) Complexes, Either cis or trans Configured

摘要: Six diiodido-diamine platinum(II) complexes, either cis or trans configured, were prepared, differing only in the nature of amine ligand (isopropylamine, dimethylamine, methylamine), and their antiproliferative properties evaluated against a panel human tumor cell lines. Both series complexes manifested pronounced cytotoxic effects, with isomers being, generally, more effective than counterparts. Cell cycle analysis revealed different modes action for these new Pt(II) respect to cisplatin. The reactivity platinum compounds number biomolecules, including cytochrome c, two sulfur containing modified amino acids, 9-ethylguanine, single strand oligonucleotide, was analyzed depth by mass spectrometry NMR spectroscopy. Interestingly, significant differences investigated toward various model biomolecules observed: particular we observed that preferentially release iodide ligands upon biomolecule binding, while may retention iodides. Such have important mechanistic implications relevant impact on respective pharmacological profiles.