title: Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes.
abstract: Three novel inosine-based dinuclear platinum complexes have been synthesized via a solid-phase strategy. In these compounds, the metal is linked both to the N-7 of the purine nucleus and to the terminal amine group of a hexylamine side chain installed on N-1. Cis- or trans- diamine as well as ethylenediamine ligands are coordinated to platinum along with a chloride. The synthesised complexes were tested against four different human tumor cell lines. One of these complexes proved to be more cytotoxic than cisplatin against the MCF7 cancer cell line in a short-term exposure assay.
authors.affiliation: Dipartimento di Chimica delle Sostanze Naturali, Università degli Studi di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy. stefano.derrico@unina.it
authors.forename: Stefano
authors.initials: S
authors.lastname: D'Errico
authors.forename: Giorgia
authors.initials: G
authors.lastname: Oliviero
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Piccialli
authors.forename: Jussara
authors.initials: J
authors.lastname: Amato
authors.forename: Nicola
authors.initials: N
authors.lastname: Borbone
authors.forename: Valentina
authors.initials: V
authors.lastname: D'Atri
authors.forename: Francesca
authors.initials: F
authors.lastname: D'Alessio
authors.forename: Rosa
authors.initials: R
authors.lastname: Di Noto
authors.forename: Francesco
authors.initials: F
authors.lastname: Ruffo
authors.forename: Francesco
authors.initials: F
authors.lastname: Salvatore
authors.forename: Gennaro
authors.initials: G
authors.lastname: Piccialli
mesh_terms: D000368:Aged; D000964:Antimetabolites, Antineoplastic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D045744:Cell Line, Tumor; D003959:Diamines / Q000737:chemistry; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D007288:Inosine / Q000737:chemistry; D015394:Molecular Structure; D009705:Nucleosides / Q000737:chemistry; D010984:Platinum / Q000737:chemistry; D060327:Solid-Phase Synthesis Techniques; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000964:Antimetabolites, Antineoplastic; D000970:Antineoplastic Agents; D003959:Diamines; D009705:Nucleosides; D010984:Platinum; D007288:Inosine