title: Influence of the π-coordinated arene on the anticancer activity of ruthenium(II) carbohydrate organometallic complexes.
abstract: The synthesis and in vitro cytotoxicity of a series of Ru(II)(arene) complexes with carbohydrate-derived phosphite ligands and various arene co-ligands is described. The arene ligand has a strong influence on the in vitro anticancer activity of this series of compounds, which correlates fairly well with cellular accumulation. The most lipophilic compound bearing a biphenyl moiety and a cyclohexylidene-protected carbohydrate is the most cytotoxic with unprecedented IC50 values for the compound class in three human cancer cell lines. This compound shows reactivity to the DNA model nucleobase 9-ethylguanine, but does not alter the secondary structure of plasmid DNA, indicating that other biological targets are responsible for its cytotoxic effect.
authors.affiliation: School of Chemical Science, The University of Auckland Auckland, New Zealand ; Institute of Inorganic Chemistry, University of Vienna Vienna, Austria ; Department of Chemistry, COMSATS Institute of Information Technology Abbottabad, Pakistan.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Hanif
authors.affiliation: Institute of Inorganic Chemistry, University of Vienna Vienna, Austria ; Research Platform "Translational Cancer Therapy Research", University of Vienna Vienna, Austria.
authors.forename: Samuel M
authors.initials: SM
authors.lastname: Meier
authors.affiliation: Institute of Inorganic Chemistry, University of Vienna Vienna, Austria ; Department of Chemistry, Moscow State University Moscow, Russia ; Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne Lausanne, Switzerland.
authors.forename: Alexey A
authors.initials: AA
authors.lastname: Nazarov
authors.affiliation: Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne Lausanne, Switzerland.
authors.forename: Julie
authors.initials: J
authors.lastname: Risse
authors.affiliation: Institute of Inorganic Chemistry, University of Vienna Vienna, Austria.
authors.forename: Anton
authors.initials: A
authors.lastname: Legin
authors.affiliation: Pharmacokinetics, Toxicology and Targeting, Research Institute of Pharmacy, University of Groningen Groningen, Netherlands.
authors.forename: Angela
authors.initials: A
authors.lastname: Casini
authors.affiliation: Institute of Inorganic Chemistry, University of Vienna Vienna, Austria ; Research Platform "Translational Cancer Therapy Research", University of Vienna Vienna, Austria.
authors.forename: Michael A
authors.initials: MA
authors.lastname: Jakupec
authors.affiliation: Institute of Inorganic Chemistry, University of Vienna Vienna, Austria ; Research Platform "Translational Cancer Therapy Research", University of Vienna Vienna, Austria.
authors.forename: Bernhard K
authors.initials: BK
authors.lastname: Keppler
authors.affiliation: School of Chemical Science, The University of Auckland Auckland, New Zealand ; Institute of Inorganic Chemistry, University of Vienna Vienna, Austria ; Research Platform "Translational Cancer Therapy Research", University of Vienna Vienna, Austria.
authors.forename: Christian G
authors.initials: CG
authors.lastname: Hartinger
keywords: anticancer activity; bioorganometallic chemistry; carbohydrates; phosphorus ligands; ruthenium arene compounds