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Synthesis,antiproliferative and mitochondrial impairment activities of bis-alkyl-amino transplatinum complexes |
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| Authors: | Lisa Dalla Via Aída N. García-Argáez Arianna Adami Silvia Grancara Pamela Martinis Antonio Toninello Daniela Belli Dell’Amico Luca Labella Simona Samaritani |
| Affiliation: | 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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