Quinizarin Gold(I) N‐Heterocyclic Carbene Complexes with Synergistic Activity Against Anthracycline‐Resistant Leukaemia Cells: Synthesis and Biological Activity Studies
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 IC$_{50}$ 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.
Institutions
- Deutsches Elektronen-Synchrotron DESY (DE)
Publication Details
- Journal
- DESY Publication Database (PUBDB) (Deutsches Elektronen-Synchrotron)
- Published
- 2025-01-01
- DOI
- https://doi.org/10.3204/pubdb-2025-01683
- Primary Topic
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Type
- article
- Field-Weighted Citation Impact
- 0.00