Publication Type Journal Article
Title New copper(i) complexes selective for prostate cancer cells
Authors J. Franco Machado Diogo Sequeira Fernanda M. Marques M. Fatima M. Piedade Maria J. Villa de Brito M. Helena Garcia A.R. Fernandes Tânia S. Morais
Groups BIOIN CCC
Journal DALTON TRANSACTIONS
Year 2020
Month September
Volume 49
Number 35
Pages 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 IC(50)values in the range 0.2-2 mu M 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 mechanismviaapoptosis/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.
DOI http://dx.doi.org/10.1039/d0dt02157a
ISBN
Publisher ROYAL SOC CHEMISTRY
Book Title
ISSN 1477-9226
EISSN 1477-9234
Conference Name
Bibtex ID ISI:000569986300017
Observations
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