Organoruthenium
compounds have been widely investigated for their anticancer activity.
Here we use one of the classic ligand classes found in organometallics,
i.e., N-heterocyclic carbenes (NHC), and coordinate them to the Ru(η6-p-cymene) scaffold as N,C-bidentate ligands substituted with a pyridyl
moiety. Introduction of different substituents gave compounds with
a wide variety of properties. We investigated their stability in solution
and in the presence of biomolecules, in vitro anticancer activity,
and cellular uptake to rationalize their biological properties in
dependence on the structure. A clear effect of their structure on
the stability in water and DMSO was found for some derivatives, which
was reflected in the reactivity to biomolecules that was determined
with selected representatives of the compound classes. The antiproliferative
activity of the compounds was widely dependent on the lipophilicity
of the N,C-bidentate ligand, but
as cellular accumulation studies revealed, lipophilicity does not
provide the full picture and additional effects must be responsible
for the anticancer activity.
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