title: New trans dichloro (triphenylphosphine)platinum(II) complexes containing N-(butyl),N-(arylmethyl)amino ligands: Synthesis, cytotoxicity and mechanism of action.
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.
authors.affiliation: Dipartimento di Scienze del Farmaco, Università degli Studi di Padova, Via F. Marzolo 5, 35131 Padova, Italy. Electronic address: lisa.dallavia@unipd.it.
authors.forename: Lisa
authors.initials: L
authors.lastname: Dalla Via
authors.affiliation: Dipartimento di Scienze del Farmaco, Università degli Studi di Padova, Via F. Marzolo 5, 35131 Padova, Italy.
authors.forename: Aída Nelly
authors.initials: AN
authors.lastname: García-Argáez
authors.affiliation: Dipartimento di Scienze Biochimiche, Università degli Studi di Roma 'La Sapienza', Piazzale Aldo Moro 5, 00185 Roma, Italy.
authors.forename: Enzo
authors.initials: E
authors.lastname: Agostinelli
authors.affiliation: Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy.
authors.forename: Daniela
authors.initials: D
authors.lastname: Belli Dell'Amico
authors.affiliation: Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy.
authors.forename: Luca
authors.initials: L
authors.lastname: Labella
authors.affiliation: Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy.
authors.forename: Simona
authors.initials: S
authors.lastname: Samaritani
mesh_terms: D000588:Amines / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D005434:Flow Cytometry; D006367:HeLa Cells; D006801:Humans; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D008024:Ligands; D009944:Organoplatinum Compounds
keywords: Antiproliferative activity; DNA topoisomerases; Transplatinum(II) complexes