Water-Soluble Salts Based on Benzofuroxan Derivatives—Synthesis and Biological Activity
Chugunova E. Matveeva V. Tulesinova A. Iskanderov E. Akylbekov N. Dobrynin A. Khamatgalimov A. Appazov N. Boltayeva L. Duisembekov B. Zhanakov M. Aleksandrova Y. Sashenkova T. Klimanova E. Allayarova U. Balakina A. Mishchenko D. Burilov A. Neganova M.
December 2022MDPI
International Journal of Molecular Sciences
2022#23Issue 23
A series of novel water-soluble salts of benzofuroxans was achieved via aromatic nucleophilic substitution reaction of 4,6-dichloro-5-nitrobenzofuroxan with various amines. The salts obtained showed good effectiveness of the pre-sowing treatment of seeds of agricultural crops at concentrations of 20–40 mmol. In some cases, the seed treatment with salts leads not only to improved seed germination, but also to the suppression of microflora growth. Additionally, their anti-cancer activityin vitrohas been researched. The compounds with morpholine fragments or a fragment of N-dimethylpropylamine, demonstrated the highest cytotoxic activity, which is in good correlation with the ability to inhibit the glycolysis process in tumor cells. Two compounds 4e and 4g were selected for further experiments using laboratory animals. It was found that the lethal dose of 50% (LD50) is 22.0 ± 1.33 mg/kg for 4e and 13.75 ± 1.73 mg/kg for 4g, i.e., compound 4e is two times less toxic than 4g, according to the mouse model in vivo. It was shown that the studied compounds exhibit antileukemia activity after a single intraperitoneal injection at doses from 1.25 to 5 mg/kg, as a result of which the average lifespan of animals with a P388 murine leukemia tumor increases from 20 to 28%. Thus, the water-soluble salts of benzofuroxans can be considered as promisingcandidates for further development, both as anti-cancer agents and as stimulants for seed germination and regulators of microflora crop growth.
acute toxicity , benzofuroxan , cancer , glycolysis , growth stimulators and regulators , phytopathological analyses of agricultural crops , water-soluble salt
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Arbuzov Institute of Organic and Physical Chemistry, FRC Kazan Scientific Center, Russian Academy of Sciences, Kazan, 420088, Russian Federation
The Kazan National Research Technological University, Kazan, 420015, Russian Federation
Kazan Federal University, Kazan, 420008, Russian Federation
Laboratory of Engineering Profile “Physical and Chemical Methods of Analysis”, Korkyt Ata Kyzylorda University, Kyzylorda, 120014, Kazakhstan
I. Zhakhaev Kazakh Scientific Research Institute of Rice Growing, Kyzylorda, 120008, Kazakhstan
Kazakh Scientific Research Institute of Plant Protection and Quarantine Named after Zhazken Zhiembayev LLP, Almaty, A30M0H6, Kazakhstan
L.N. Gumilyov Eurasian National University, Astana, 010008, Kazakhstan
Institute of Physiologically Active Compounds at Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, 142432, Russian Federation
Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry—RAS, Chernogolovka, 142432, Russian Federation
Faculty of Fundamental Physical-Chemical Engineering, M.V. Lomonosov—MSU, Moscow, 119991, Russian Federation
Biomedical Institute of the Scientific and Educational Center, Moscow Regional State University, Chernogolovka, Mytishchi, 141014, Russian Federation
Arbuzov Institute of Organic and Physical Chemistry
The Kazan National Research Technological University
Kazan Federal University
Laboratory of Engineering Profile “Physical and Chemical Methods of Analysis”
I. Zhakhaev Kazakh Scientific Research Institute of Rice Growing
Kazakh Scientific Research Institute of Plant Protection and Quarantine Named after Zhazken Zhiembayev LLP
L.N. Gumilyov Eurasian National University
Institute of Physiologically Active Compounds at Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry
Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry—RAS
Faculty of Fundamental Physical-Chemical Engineering
Biomedical Institute of the Scientific and Educational Center
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