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Quinizarin Gold(I) N-Heterocyclic Carbene Complexes with Synergistic Activity Against Anthracycline-Resistant
Axel Steinbrueck1, Matthew L Reback1, Christoph Rumancev2
1Faculty of Chemistry and Biochemistry, Inorganic Chemistry I - Bioinorganic Chemistry, Ruhr University Bochum, Universitaetsstrasse 150, 44801, Bochum, Germany.
Abstract:
New, asymmetric quinizarin-Au(I)-NHC complexes were designed, isolated, and fully characterised including by single crystal X-ray crystallography. Cytotoxicity studies showed effective growth inhibition in HeLa cervical cancer cells with IC50 values ranging from 2.4 μM to 5.3 μM. The successful cellular uptake was evidenced by X-ray fluorescence imaging on cryo-preserved whole HeLa cells and the sub-cellular localisation was monitored by live-cell fluorescence microscopy. Notably, complex 2 b showed circumvention of acquired anthracycline resistance in K562 leukaemia cells as well as synergistic activity with doxorubicin against both wild-type and anthracycline-resistant Nalm-6 leukaemia cells. Interestingly, sub-cellular localisation towards mitochondria proved to be more important than the compounds' overall cytotoxicity for potent antiproliferative activity and to achieve effective resistance circumvention.
