Anticancer activity of ruthenium(II) polypyridine complexes bearing pyrrolidine substituents

• High cytotoxicity of Ru(II) complexes with pyrrolidines substituents was obtained.
• Correlation between oxidation potential and cytotoxicity was found.
• ROS formation was proposed as one of possible mechanism for cell death.
• The interaction with biomacromolecules (albumin, DNA) is discussed.

A set of homoleptic ruthenium polypyridine (bipyridine and terpyridine) complexes flanked with several electron-donating pyrrolidine moieties has been characterized and the anticancer activity was evaluated toward human lung adenocarcinoma epithelial (A549) and murine colon carcinoma (CT26). Good antiproliferative effects were observed with an IC50 ranging from ca. 4 to 21 μM against both cell lines. Dependence was found between the cytotoxicity, the lipophilicity and the RuII/RuIII oxidation potential. All the studied compounds interacted quite well with albumin while the interaction with DNA was marginal. The biological studies revealed that the ruthenium complexes induced the ROS overproduction which might be one but not the only way of cell death induction.

Homoleptic ruthenium polypyridine complexes bearing pyrrolidine moieties showed good antiproliferative effects with an IC50 ranging from 4 to 21 μM against A549 and CT26 cancer cell lines.Figure optionsDownload as PowerPoint slide