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Start Over Author "SOLARI, E." Topic antineoplastic agents
2 results on '"SOLARI, E."'

1. Unsymmetrical Trifluoromethyl Methoxyphenyl β-Diketones: Effect of the Position of Methoxy Group and Coordination at Cu(II) on Biological Activity.

Author

Khamidullina LA, Puzyrev IS, Burygin GL, Dorovatovskii PV, Zubavichus YV, Mitrofanova AV, Khrustalev VN, Timofeeva TV, Slepukhin PA, Tobysheva PD, Pestov AV, Solari E, Tskhovrebov AG, and Nenajdenko VG

Subjects
Animals, Anti-Bacterial Agents chemical synthesis, Anti-Bacterial Agents chemistry, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Cell Proliferation drug effects, Cell Survival drug effects, Chlorocebus aethiops, Coordination Complexes chemical synthesis, Coordination Complexes chemistry, Copper chemistry, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, HeLa Cells, Humans, Ketones chemistry, Microbial Sensitivity Tests, Molecular Docking Simulation, Molecular Structure, Structure-Activity Relationship, Vero Cells, Anti-Bacterial Agents pharmacology, Antineoplastic Agents pharmacology, Coordination Complexes pharmacology, Copper pharmacology, Escherichia coli drug effects, Ketones pharmacology, Staphylococcus aureus drug effects
Abstract

Copper(II) complexes with 1,1,1-trifluoro-4-(4-methoxyphenyl)butan-2,4-dione (H L1 ) were synthesized and characterized by elemental analysis, FT-IR spectroscopy, and single crystal X-ray diffraction. The biological properties of H L1 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 H L1 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.

Published
2021
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2. Unsymmetrical Trifluoromethyl Methoxyphenyl β-Diketones: Effect of the Position of Methoxy Group and Coordination at Cu(II) on Biological Activity

Author

Khamidullina, L. A., Puzyrev, I. S., Burygin, G. L., Dorovatovskii, P. V., Zubavichus, Y. V., Mitrofanova, A. V., Khrustalev, V. N., Timofeeva, T. V., Slepukhin, P. A., Tobysheva, P. D., Pestov, A. V., Solari, E., Tskhovrebov, A. G., and Nenajdenko, V. G.

Subjects
DOSE RESPONSE, DRUG EFFECT, ANTIINFECTIVE AGENT, COORDINATION COMPOUND, HELA CELLS, MOLECULAR STRUCTURE, DIKETONATES, ANTINEOPLASTIC AGENT, MICROBIAL SENSITIVITY TESTS, DRUG SCREENING, HELA CELL LINE, COPPER, MOLECULAR DOCKING SIMULATION, ANTINEOPLASTIC AGENTS, SYNTHESIS, CYTOTOXIC ACTIVITY, VERO CELL LINE, KETONE, CHEMISTRY, KETONES, MOLECULAR DOCKING, DOSE-RESPONSE RELATIONSHIP, DRUG, STAPHYLOCOCCUS AUREUS, STRUCTURE-ACTIVITY RELATIONSHIP, ANTIMICROBIAL ACTIVITY, CHEMICAL STRUCTURE, MICROBIAL SENSITIVITY TEST, ANIMALS, HUMAN, HUMANS, ANIMAL, DRUG SCREENING ASSAYS, ANTITUMOR, COORDINATION COMPLEXES, ANTI-BACTERIAL AGENTS, CELL PROLIFERATION, VERO CELLS, ANTICANCER AGENTS, CELL SURVIVAL, ESCHERICHIA COLI, STRUCTURE ACTIVITY RELATION, COPPER(II), CHLOROCEBUS AETHIOPS
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. © 2021, MDPI. All rights reserved. This work was funded by RFBR and Sverdlovsk region (project numbers 20-43-660042 and 20-53-00006) and supported by the basic theme of the Russian Academy of Sciences (state registration no. AAAA-A19-119011790132-7 and project no. AAAA-A19-119012490006-1). XRD experiments and analytical studies were carried out using the equipment of the Center for Joint Use “Spectroscopy and Analysis of Organic Compounds” at the Postovsky Institute of Organic Synthesis UB RAS. X-ray study was supported by the U.S. National Science Foundation (Grant DMR-1523611 PREM). The cytotoxicity assay was carried out at the “Simbioz” Center for the Collective Use of Research Equipment in the Field of Physical–Chemical Biology and Nanobiotechnology at IBPPM RAS. This work has been supported by the RUDN University Strategic Academic Leadership Program.

Published
2021

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