Abstract
Copper(II) complexes with 1,1,1-trifluoro-4-(4-methoxyphenyl)butan-2,4-dione (HL1) were synthesized and characterized by elemental analysis, FT-IR spectroscopy, and single crystal X-ray diffraction. The biological properties of HL1 and cis-[Cu(L1)2(DMSO)] (3) were examined against Gram-positive and Gram-negative bacteria and opportunistic unicellular fungi. The cytotoxicity was estimated towards the HeLa and Vero cell lines. Complex 3 demonstrated antibacterial activity towards S. aureus comparable to that of streptomycin, lower antifungal activity than the ligand HL1 and moderate cytotoxicity. The bioactivity was compared with the activity of compounds of similar structures. The effect of changing the position of the methoxy group at the aromatic ring in the ligand moiety of the complexes on their antimicrobial and cytotoxic activity was explored. We propose that complex 3 has lower bioavailability and reduced bioactivity than expected due to strong intermolecular contacts. In addition, molecular docking studies provided theoretical information on the interactions of tested compounds with ribonucleotide reductase subunit R2, as well as the chaperones Hsp70 and Hsp90, which are important biomolecular targets for antitumor and antimicrobial drug search and design. The obtained results revealed that the complexes displayed enhanced affinity over organic ligands. Taken together, the copper(II) complexes with the trifluoromethyl methoxyphenyl-substituted β-diketones could be considered as promising anticancer agents with antibacterial properties.
Highlights
Cancer is the second leading cause of death globally according to a surveillance report compiled by WHO [1]
We have synthesized and characterized for the first time Cu(II) complexes based on trifluoromethyl- and methoxyphenyl-containing β-diketones
Docking studies generally pointed to the enhanced affinity of metal complexes binding to the target sites over the organic ligands and the findings agree with the effect towards eukaryotic cells
Summary
Cancer is the second leading cause of death globally (just after cardiovascular diseases) according to a surveillance report compiled by WHO [1]. The major cancer treatment options include surgery, radiation therapy, and chemotherapy. Anti-tumor drugs used for chemotherapy often induce undesired side effects [2] with damage to the rapidly self-renewing cells of the hematopoietic and immunocompetent organs being dominant. Neutropenia is a frequently occurring sequela of drug therapy, which enhances the probability of the occurrence of life-threatening bloodstream infections requiring stationary treatment in a hospital, including antibiotic courses [3,4]. The development of neutropenia is promoted by various factors, such as concomitant immunodeficiency (associated with the tumor, immunosuppressive therapy applied, or repeated surgical interventions) and chronic deceases [5]. Many lethal cases with immune-compromised cancer patients are due to hospital-acquired infections [6]
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