Novel Copper(II) Coordination Compounds Containing Pyridine Derivatives of N4-Methoxyphenyl-Thiosemicarbazones with Selective Anticancer Activity
2024

Copper(II) Coordination Compounds with Anticancer Activity

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Author Information

Author(s): Rusnac Roman, Garbuz Olga, Kravtsov Victor, Melnic Elena, Istrati Dorin, Tsapkov Victor, Poirier Donald, Gulea Aurelian

Primary Institution: Moldova State University

Hypothesis

The incorporation of methoxy-phenyl fragments into thiosemicarbazone skeletons will enhance their anticancer activity and selectivity.

Conclusion

The synthesized copper(II) coordination compounds exhibited significant anticancer activity, often surpassing that of doxorubicin and cisplatin.

Supporting Evidence

  • Most compounds demonstrated selective anticancer activity superior to doxorubicin.
  • All ligands showed high antiproliferative activity against HL-60 cells, with IC50 values between 0.01 and 0.06 µM.
  • Coordination of copper(II) with ligands HL1 and HL3 notably enhanced antiproliferative activity, lowering the IC50 to 0.03 µM.
  • All tested ligands exhibited greater antioxidant activity compared to Trolox, with some ligands showing activity up to 12.3 times higher.
  • Toxicity studies indicated low toxicity for the ligands, generally less than doxorubicin, with LC50 values ranging from 13 to 90 µM.

Takeaway

Scientists created new compounds that can fight cancer better than some existing drugs. They found that adding certain groups to these compounds makes them work even better.

Methodology

The study involved synthesizing and characterizing thiosemicarbazone compounds and evaluating their anticancer activity against various cancer cell lines using IC50 values.

Limitations

The study primarily focused on in vitro testing, which may not fully represent in vivo efficacy and safety.

Digital Object Identifier (DOI)

10.3390/molecules29246002

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