New trans dichloro (triphenylphosphine)platinum(II) complexes containing N-(butyl),N-(arylmethyl)amino ligands: Synthesis,cytotoxicity and mechanism of action |
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Institution: | 1. School of Chemical Sciences, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand;2. School of Biological Sciences, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand;3. Auckland Cancer Society Research Centre, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand |
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Abstract: | Some new platinum(II) complexes have been prepared, of general formula trans-PtCl2(PPh3){NH(Bu)CH2Ar}], where the dimension of the Ar residue in the secondary amines has been varied from small phenyl to large pyrenyl group. The obtained complexes, tested in vitro towards a panel of human tumor cell lines showed an interesting antiproliferative effect on both cisplatin-sensitive and -resistant cells. For the most cytotoxic derivative 2a the investigation on the mechanism of action highlighted the ability to induce apoptosis on resistant cells and interestingly, to inhibit the catalytic activity of topoisomerase II. |
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Keywords: | Transplatinum(II) complexes Antiproliferative activity DNA topoisomerases |
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