New copper(I) complexes selective for prostate cancer cells
- Citation:
- Machado, JF, Sequeira D, Marques F, Piedade MFM, Villa de Brito MJ, Helena Garcia M, Fernandes AR, Morais TS. 2020. New copper(I) complexes selective for prostate cancer cells, 2020. Dalton Trans. 49(35):12273-12286.
Abstract:
A new family of eighteen Cu(i) complexes of the general formula [Cu(PP)(LL)][BF4], where PP is a phosphane ligand and LL represents an N,O-heteroaromatic bidentate ligand, has been synthesized and fully characterized by classical analytical and spectroscopic methods. Five complexes of this series were also characterized by single crystal X-ray diffraction studies. The cytotoxicity of all compounds was evaluated in breast (MCF7) and prostate (LNCap) human cancer cells and in a normal prostate cell line (RWPE). In general, all compounds showed higher cytotoxicity for the prostate cancer cells than for the breast cells, with IC50 values in the range 0.2-2 muM after 24 h of treatment. The most cytotoxic compound, [Cu(dppe)(2-ap)][BF4] (16), where dppe = 1,2-bis(diphenylphosphano) ethane and 2-ap = 2-acetylpyridine, showed a high level of cellular internalization, generation of intracellular ROS and activation of the cell death mechanism via apoptosis/necrosis. Owing to its high cytotoxic activity for LNCap cells, being 70-fold higher than that for normal prostate cells (RWPE), complex (16) was found to be the most promising for further research in prostate cancer models.
Notes:
Machado, Joao FrancoSequeira, Diogo
Marques, Fernanda
Piedade, M Fatima M
Villa de Brito, Maria J
Helena Garcia, M
Fernandes, Alexandra R
Morais, Tania S
eng
England
Dalton Trans. 2020 Sep 15;49(35):12273-12286. doi: 10.1039/d0dt02157a.