title: Cisplatin and its dibromido analogue: a comparison of chemical and biological profiles.
abstract: The dibromido analogue of cisplatin, cis-PtBr2(NH3)2 (cisPtBr2 hereafter), has been prepared and characterised. Its solution behaviour in standard phosphate buffer, at pH 7.4, was investigated spectrophotometrically and found to reproduce quite closely that of cisplatin; indeed, progressive sequential release of the two halide ligands typically occurs as in the case of cisplatin, with a roughly similar kinetics. Afterward, patterns of reactivity toward model proteins and standard ctDNA were explored and the nature of the resulting interactions elucidated. The antiproliferative properties were then evaluated in four representative cancer cell lines, namely A549 (human lung cancer), HCT116 (human colon cancer), IGROV-1 (human ovarian cancer) and FLG 29.1 (human acute myeloid leukaemia). Cytotoxic properties in line with those of cisplatin were highlighted. From these studies an overall chemical and biological profile emerges for cisPtBr2 closely matching that of cisplatin; the few slight, but meaningful differences that were underscored might be advantageously exploited for clinical application.
authors.affiliation: Laboratory of Metals in Medicine (MetMed), Department of Chemistry, University of Florence, Via della Lastruccia 3, 50019, Sesto Fiorentino, Italy. tiziano.marzo@unifi.it.|Department of Chemistry and Industrial Chemistry, University of Pisa, via Moruzzi, 3, 56124, Pisa, Italy. tiziano.marzo@unifi.it.
authors.forename: Tiziano
authors.initials: T
authors.lastname: Marzo
authors.affiliation: Department of Experimental and Clinical Medicine, University of Florence, Viale GB Morgagni 50, 50134, Florence, Italy.
authors.forename: Gianluca
authors.initials: G
authors.lastname: Bartoli
authors.affiliation: Department of Chemistry and Industrial Chemistry, University of Pisa, via Moruzzi, 3, 56124, Pisa, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Gabbiani
authors.affiliation: Department of Chemistry and Industrial Chemistry, University of Pisa, via Moruzzi, 3, 56124, Pisa, Italy.
authors.forename: Gennaro
authors.initials: G
authors.lastname: Pescitelli
authors.affiliation: Department of Chemistry, University of Florence, Via della Lastruccia 3, 50019, Sesto Fiorentino, Italy.
authors.forename: Mirko
authors.initials: M
authors.lastname: Severi
authors.affiliation: Department of Experimental and Clinical Medicine, University of Florence, Viale GB Morgagni 50, 50134, Florence, Italy.
authors.forename: Serena
authors.initials: S
authors.lastname: Pillozzi
authors.affiliation: Mass Spectrometry Centre (CISM), University of Florence, Via U. Schiff 6, 50019, Sesto Fiorentino, Italy.
authors.forename: Elena
authors.initials: E
authors.lastname: Michelucci
authors.affiliation: Laboratory of Metals in Medicine (MetMed), Department of Chemistry, University of Florence, Via della Lastruccia 3, 50019, Sesto Fiorentino, Italy.
authors.forename: Benedetta
authors.initials: B
authors.lastname: Fiorini
authors.affiliation: Department of Experimental and Clinical Medicine, University of Florence, Viale GB Morgagni 50, 50134, Florence, Italy.
authors.forename: Annarosa
authors.initials: A
authors.lastname: Arcangeli
authors.affiliation: Department of Inorganic Chemistry, Universidad Autonóma de Madrid, C/Francisco Tomás y Valiente 7, 28049, Madrid, Spain.
authors.forename: Adóracion G
authors.initials: AG
authors.lastname: Quiroga
authors.affiliation: Laboratory of Metals in Medicine (MetMed), Department of Chemistry, University of Florence, Via della Lastruccia 3, 50019, Sesto Fiorentino, Italy. luigi.messori@unifi.it.
authors.forename: Luigi
authors.initials: L
authors.lastname: Messori
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001965:Bromides / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002945:Cisplatin / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D000091344:Filaggrin Proteins; D045325:HCT116 Cells; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D001965:Bromides; C000717249:FLG protein, human; D000091344:Filaggrin Proteins; D008024:Ligands; D002945:Cisplatin
keywords: Cancer; Circular dichroism; Cisplatin analogues; Mass spectrometry; Platinum