AUTHOR=Hanif Muhammad , Meier Samuel , Nazarov Alexey , Risse Julie , Legin Anton , Casini Angela , Jakupec Michael A., Keppler Bernhard K., Hartinger Christian G.

TITLE=Influence of the π-coordinated arene on the anticancer activity of ruthenium(II) carbohydrate organometallic complexes

JOURNAL=Frontiers in Chemistry

VOLUME=1

YEAR=2013

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2013.00027

DOI=10.3389/fchem.2013.00027

ISSN=2296-2646

ABSTRACT=<p>The synthesis and <italic>in vitro</italic> cytotoxicity of a series of Ru<sup>II</sup>(arene) complexes with carbohydrate-derived phosphite ligands and various arene co-ligands is described. The arene ligand has a strong influence on the <italic>in vitro</italic> 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 IC<sub>50</sub> 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.</p>