AI Article Synopsis
- New quinizarin-Au(I)-NHC complexes were developed and fully characterized, demonstrating effective growth inhibition in HeLa cervical cancer cells with IC values between 2.4 and 5.3 μM.
- Cytotoxicity studies showed that complex 2 b could overcome anthracycline resistance in K562 leukemia cells and worked synergistically with doxorubicin against both sensitive and resistant leukemia cells.
- The study highlighted that localizing these complexes to mitochondria was crucial for their antiproliferative effects and ability to counteract drug resistance, rather than just overall cytotoxicity.
Article 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 IC 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.
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| http://dx.doi.org/10.1002/chem.202404147 | DOI Listing |
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