Ferrocene as a redox-active auxiliary for novel anticancer agents

Two sets of novel ferrocene-conjugated compounds have been developed as novel anticancer agents. In the first case these are ferrocene (Fc) functionalized coumarin and anthraquinone. Electron paramagnetic resonance (EPR) spin-trapping studies show that the Fc group has an intrinsic ability to generate reactive oxygen species (ROS), with, in vitro studies confirming this also occurs in MCF-7 cancer cells. The Fc-coumarin compound showed promising cytotoxic activity. The second case of compounds revolve around Fc-conjugated derivatives of anticancer Ru(II)-arenes. DNA interaction studies displayed promising results for the Fc-Ru(II) heteronuclear bimetallic compounds. However, although in vitro cytotoxicity studies showed promising activity for the parent compounds, the Fc-conjugated complexes were less active. Cellular uptake studies using ICP-MS were performed to confirm Fc conjugation negatively impacted on internalization, likely due to increased lipophilicity.