Copper(I) Complexes as Dual Anticancer and Antiparasitic Agents

Copper(I) Complexes as Dual Anticancer and Antiparasitic Agents

Author: ChemMedChem

Parasitic infections and cancers have some features in common. Anticancer drugs such as cisplatin have been found to also have antiparasitic effects, and some antiparasitic drugs such as artemisinin can be used in cancer therapy. There is an ongoing need for the development of more efficient antitumor and antiparasitic agents. Metal complexes, e.g., involving copper, are promising candidates in this context. However, only a small number of known copper complexes with anticancer and antiparasitic potential include Cu(I) as the central ion.

Tânia S. Morais, Universidade de Lisboa, Portugal, and colleagues have synthesized a new family of Cu(I) complexes with different combinations of two phosphane ligands and two bioactive thiosemicarbazone derivatives (pictured below). The complexes show in-vitro antiparasitic/anticancer activity and selectivity over healthy human cells. They were prepared via reactions of the precursor complexes [Cu(dppe)(NCCH3)2][BF4] (dppe = 1,2-bis(diphenylphosphano)ethane) or [Cu(PPh3)2(NCCH3)2][BF4] (PPh3 = triphenylphosphane) with 4-(methyl)-1-(5-nitrofurfurylidene) thiosemicarbazide or 4-(ethyl)-1-(5-nitrofurfurylidene)thiosemicarbazide at room temperature.



The researchers found that the new compounds are more active than the benchmark drugs nifurtimox and cisplatin against the trypomastigote form of Trypanosoma cruzi (a parasite that causes Chagas disease) and the chemoresistant PC3 prostate cancer cell line. The complexes induce cell death through apoptosis without generating oxidative stress. They also show some selectivity for parasite/cancer cells over healthy cells. The team found that the phosphane co-ligand plays an important role in the activity and selectivity of the complexes. The copper(I) complexes could be useful for further development as new dual-action drugs for clinical applications.


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