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Synthesis,antiproliferative and mitochondrial impairment activities of bis-alkyl-amino transplatinum complexes
Authors:Lisa Dalla Via  Aída N García-Argáez  Arianna Adami  Silvia Grancara  Pamela Martinis  Antonio Toninello  Daniela Belli Dell’Amico  Luca Labella  Simona Samaritani
Institution:1. Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy;2. Department of Chemical Sciences, University of Padova, Via F. Marzolo 1, 35131 Padova, Italy;3. Department of Biomedical Sciences, University of Padova, Via G. Colombo 3, 35121 Padova, Italy;4. Department of Chemistry and Industrial Chemistry, University of Pisa, Via Risorgimento 35, 56126 Pisa, Italy
Abstract:A convenient synthetic route and the characterization of complexes trans-PtCl2(L)(PPh3)] (L = Et2NH (2), (PhCH2)2NH (3), (HOCH2CH2)2NH) (4) are reported. The antiproliferative activity was evaluated on three human tumor cell lines. The investigation on the mechanism of action highlighted for the most active complex 4 the capacity to affect mitochondrial functions. In particular, both the induction of the mitochondrial permeability transition phenomenon and an aspecific membrane damage occurred, depending on concentration.
Keywords:Transplatinum complexes  Antiproliferative activity  Mitochondria  Mitochondrial permeability transition  Oxidative stress
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