1. New quaternary ammonium camphor derivatives and their antiviral activity, genotoxic effects and cytotoxicity
- Author
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Capital O Cyrilliclga I Yarovaya, Vladimir V. Zarubaev, Capital A Cyrillicndrey G Pokrovsky, Pavel Anfimov, Tatiana S. Tretiak, Oleg I. Kiselev, Capital Em Cyrillicichail A Pokrovsky, Nariman F. Salakhutdinov, V. A. Lavrinenko, Capital A Cyrillicndrey V Shernyukov, A. S. Sokolova, and Anatoly B. Beklemishev
- Subjects
Cell Survival ,Stereochemistry ,Cytotoxicity ,Clinical Biochemistry ,Pharmaceutical Science ,medicine.disease_cause ,Antiviral Agents ,Biochemistry ,Article ,Virus ,Madin Darby Canine Kidney Cells ,Viral Matrix Proteins ,Bridged Bicyclo Compounds ,Camphor ,chemistry.chemical_compound ,Dogs ,Influenza A Virus, H1N1 Subtype ,Cell Line, Tumor ,Imine derivatives ,Drug Discovery ,Escherichia coli ,medicine ,Animals ,Humans ,Ammonium ,Binding site ,Molecular Biology ,ComputingMethodologies_COMPUTERGRAPHICS ,Binding Sites ,Mutagenicity Tests ,Organic Chemistry ,Antivirals ,Influenza ,Protein Structure, Tertiary ,Molecular Docking Simulation ,Quaternary Ammonium Compounds ,chemistry ,Toxicity ,Molecular Medicine ,Genotoxicity - Abstract
Graphical abstract, The synthesis and biological evaluation of a novel series of dimeric camphor derivatives are described. The resulting compounds were studied for their antiviral activity, cyto- and genotoxicity. Compounds 3a and 3d in which the quaternary nitrogen atoms are separated by the C5H10 and С9H18 aliphatic chain, exhibited the highest efficiency as an agent inhibiting the reproduction of the influenza virus A(H1N1)pdm09. The cytotoxicity data of compounds 3 and 4 revealed their moderate activity against malignant cell lines; compound 3f had the highest activity for the CEM-13 cells. These results show close agreement with the data of independent studies on toxicity of these compounds, in particular that the toxicity of compounds strongly depends on spacer length.
- Published
- 2013
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