title: A new design for nucleolipid-based Ru(III) complexes as anticancer agents.
abstract: In continuation with our studies concerning the synthesis, characterization and biological evaluation of nucleolipidic Ru(III) complexes, a novel design for this family of potential anticancer agents is presented here. As a model compound, a new uridine-based nucleolipid has been prepared, named HoUrRu, following a simple and versatile synthetic procedure, and converted into a Ru(III) salt. Stable formulations of this highly functionalized Ru(III) complex have been obtained by co-aggregation with either the zwitterionic lipid POPC or the cationic DOTAP, which have been subjected to an in-depth microstructural characterization, including DLS, SANS and EPR measurements. The in vitro bioactivity profile of HoUrRu, as a pure compound or in formulation with POPC or DOTAP, reveals high antiproliferative activity against MCF-7 and WiDr human cancer cell lines.
authors.affiliation: Department of Chemical Sciences, University of Napoli "Federico II", Complesso Universitario di Monte Sant'Angelo, via Cintia 21, I-80126, Napoli, Italy. daniela.montesarchio@unina.it.
authors.forename: Daniela
authors.initials: D
authors.lastname: Montesarchio
authors.forename: Gaetano
authors.initials: G
authors.lastname: Mangiapia
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Vitiello
authors.forename: Domenica
authors.initials: D
authors.lastname: Musumeci
authors.forename: Carlo
authors.initials: C
authors.lastname: Irace
authors.forename: Rita
authors.initials: R
authors.lastname: Santamaria
authors.forename: Gerardino
authors.initials: G
authors.lastname: D'Errico
authors.forename: Luigi
authors.initials: L
authors.lastname: Paduano
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D010713:Phosphatidylcholines / Q000737:chemistry* / Q000494:pharmacology; D000644:Quaternary Ammonium Compounds / Q000737:chemistry* / Q000494:pharmacology; D012428:Ruthenium / Q000737:chemistry* / Q000494:pharmacology; D014529:Uridine / Q000031:analogs & derivatives* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D005229:Fatty Acids, Monounsaturated; D010713:Phosphatidylcholines; D000644:Quaternary Ammonium Compounds; D012428:Ruthenium; C070046:1,2-dioleoyloxy-3-(trimethylammonium)propane; C028694:1-palmitoyl-2-oleoylphosphatidylcholine; D014529:Uridine