Synthesis and cytotoxicity of 7,8-dihalopyrido[1,2-a]benzimidazole-6,9-dione and its 1,2,3,4-tetrahydro analogue |
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| Institution: | 1. P. G. Demidov Yaroslavl State University, 150003 Yaroslavl, Russian Federation;2. Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, 142432 Chernogolovka, Moscow Region, Russian Federation;1. Faculty of Chemistry, Tomsk State University, 634050 Tomsk, Russian Federation;2. Research Institute of Medical Genetics, 634050 Tomsk, Russian Federation;3. Siberian State Medical University, 634055 Tomsk, Russian Federation;4. Tomsk Polytechnic University, 634050 Tomsk, Russian Federation;1. I. Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, 620990 Ekaterinburg, Russian Federation;2. Perm National Research Polytechnic University, 614990 Perm, Russian Federation;1. Department of Chemistry, Voronezh State University, 394018 Voronezh, Russian Federation;2. Faculty of Science, Tishreen University, 2237 Latakia, Syrian Arab Republic;1. Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;2. A. N. Belozersky Institute of Physico-Chemical Biology, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;1. National Research Center ‘Kurchatov Institute’, 123182 Moscow, Russian Federation;2. A. V. Shubnikov Institute of Crystallography, FSRC ‘Crystallography and Photonics’, Russian Academy of Sciences, 119333 Moscow, Russian Federation;3. A. S. Loginov Moscow Clinical Scientific Center, 111123 Moscow, Russian Federation |
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| Abstract: | An efficient synthesis of 8-bromo-7-chloropyrido1,2-a]-benzimidazole-6,9-dione and its 1,2,3,4-tetrahydro analogue from N-(4-chloro-2-nitrophenyl)pyridinium chloride has been accomplished. The study for antitumour activity against cancer cell lines such as A549, SH-SY5Y, Hep-2, HeLa and MCF-7 revealed that the cytotoxic effect of the compounds obtained was several times higher than that of Mitomycin C. |
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| Keywords: | 2-bromo-3-chloro-1 4-benzoquinones intramolecular reductive reactions hetero- cyclization flow-through catalytic hydrogenation prooxidant activity cytotoxicity |
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