Structure activity relationships investigation in a class of new platinum complexes with 3.5-disubstituted hydantoins and spiro-5’-hydantoins

personАвтори: A. Bakalova, G. Momekov


Twenty two new Pt(II) and Pt(V) complexes with 3.5-disubstituted hydantoins and spiro-5’-hydantoins were synthesized and studied. Pt(II) complexes have been prepared as structural analogues of cisplatin with different carrier ligands. Pt(IV) complexes were with general formula cis-[PtL2Cl4]. Platinum complexes were studied in vitro for cytotoxic activity on panel of human tumor cell lines. The cytotoxicity of new Pt(II) complexes were compared with those of Pt(IV) complexes and the reference cytotoxic drugcisplatin. The tested platinumagentsdisplayed concentration dependent cytotoxic activity at micromolar concentrations. Among the series a Pt(II) complex with 3-benzyl-5-methyl-5-(4-pyridyl)hydantoin as carrier ligand proved to be the most active analogue, whose relative potency in SKW-3 cell linewas similar to that of the reference antineoplastic drug cisplatin.

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