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Issue 16, 2019
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Copper(II) complexes based on tripodal pyridyl amine derivatives as efficient anticancer agents

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Abstract

The complexes [Cu(TPA)Cl]ClO4·½H2O (1-ClO4), [Cu(6-MeTPA)Cl]ClO4/PF6 (2-ClO4/2-PF6), [Cu(6-Me2TPA)Cl]PF6 (3-PF6), [Cu(BPQA)Cl]ClO4/PF6 (4-ClO4/4-PF6), [Cu(BPQA)Cl]ClO4/PF6 (4-ClO4/4-PF6), [Cu(BQPA)Cl]ClO4/PF6 (5-ClO4/PF6), [Cu(L1)Cl]ClO4/PF6 (6-ClO4/6-PF6), [Cu(L2)Cl]ClO4 (7-ClO4) and [Cu(L3)Cl]ClO4 (8-ClO4) have been synthesized and structurally characterized by spectroscopic techniques and single X-ray crystallography. The in vitro cytotoxicity of the prepared Cu(II) complexes was evaluated against A2780 (ovarian), A2780R (cisplatin-resistant variant) and MCF7 (breast cancer) human cancer cell lines. Overall, the complexes revealed significant-to-moderate cytotoxicity, with the best results obtained for the complexes [Cu(BQPA)Cl]ClO4 (5-ClO4) and [Cu(BQPA)Cl]PF6 (5-PF6), showing IC50 values within the range of 4.7–10.8 μM. The ability of the most cytotoxic complexes to cleave DNA under different conditions and the mechanisms underlying this activity were assessed by means of agarose gel electrophoresis.

Graphical abstract: Copper(ii) complexes based on tripodal pyridyl amine derivatives as efficient anticancer agents

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Publication details

The article was received on 05 Jan 2019, accepted on 18 Mar 2019 and first published on 18 Mar 2019


Article type: Paper
DOI: 10.1039/C9NJ00061E
New J. Chem., 2019,43, 6186-6196

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    Copper(II) complexes based on tripodal pyridyl amine derivatives as efficient anticancer agents

    S. S. Massoud, F. R. Louka, A. F. Tusa, N. E. Bordelon, R. C. Fischer, F. A. Mautner, J. Vančo, J. Hošek, Z. Dvořák and Z. Trávníček, New J. Chem., 2019, 43, 6186
    DOI: 10.1039/C9NJ00061E

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