Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 24, Issue 13, Pages 2929-2937Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.04.067
Keywords
Transplatinum(II) complexes; Antiproliferative activity; DNA topoisomerases
Funding
- Universita degli Studi di Padova-Progetti di Ricerca di Ateneo [CPDA109877]
- Universita di Pisa-Progetti di Ricerca di Ateneo [PRA_2015_0055]
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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. (C) 2016 Elsevier Ltd. All rights reserved.
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