title: A first-in-class and a fished out anticancer platinum compound: cis-[PtCl2(NH3)2] and cis-[PtI2(NH3)2] compared for their reactivity towards DNA model systems.
abstract: Contrary to what was believed for many years, cis-PtI2(NH3)2, the diiodido analogue of cisplatin, displays high in vitro antiproliferative activity toward a set of tumour cell lines, overcoming resistance to cisplatin in a platinum-resistant cancer cell line. In the context of a general reappraisal of iodinated Pt(ii) derivatives, aiming at a more systematic evaluation of their chemical and biological profiles, here we report on the reactivity of cis-PtI2(NH3)2 with selected DNA model systems, in single, double strand or G-quadruplex form, using cisplatin as a control. A combined approach has been exploited in this study, including circular dichroism (CD), UV-visible spectroscopy and electrospray mass spectrometry (ESI-MS) analyses. The data reveal that cis-PtI2(NH3)2 shows an overall reactivity towards the investigated oligonucleotides significantly higher than cisplatin.
authors.affiliation: Department of Chemical Sciences, University of Napoli Federico II, Via Cintia, 21, I-80126 Napoli, Italy. daniela.montesarchio@unina.it.
authors.forename: Domenica
authors.initials: D
authors.lastname: Musumeci
authors.forename: Chiara
authors.initials: C
authors.lastname: Platella
authors.forename: Claudia
authors.initials: C
authors.lastname: Riccardi
authors.forename: Antonello
authors.initials: A
authors.lastname: Merlino
authors.forename: Tiziano
authors.initials: T
authors.lastname: Marzo
authors.forename: Lara
authors.initials: L
authors.lastname: Massai
authors.forename: Luigi
authors.initials: L
authors.lastname: Messori
authors.forename: Daniela
authors.initials: D
authors.lastname: Montesarchio
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism*; D045744:Cell Line, Tumor; D002942:Circular Dichroism; D002945:Cisplatin / Q000737:chemistry; D056831:Coordination Complexes / Q000737:chemistry / Q000378:metabolism*; D004247:DNA / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D007536:Isomerism; D010984:Platinum / Q000737:chemistry*; D021241:Spectrometry, Mass, Electrospray Ionization; D013056:Spectrophotometry, Ultraviolet; D044366:Transition Temperature
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D010984:Platinum; D004247:DNA; D002945:Cisplatin