Potassium 7,8-dicarba-nido-undecaborate was thiocyanated by nondiaphragm electrolysis. The salt Me4N+[9-SCN-7,8-C2B9H11]− was isolated and converted into the trimethylammonium salt using ion-exchange. Methods for the synthesis of water-soluble sodium 7,8-dicarba-nido-undecaborate and its biphasic iodination (for 131I introduction) were developed. Thus, the synthesis and analysis of the radioactive iodine-labeled sodium salt of 11-(131I)-9-thiocyanato-7,8-dicarba-nido-undecaborate were proposed and carried out. The toxicity of the synthesized compound was evaluated. It was established that 100 and 75 mg/kg doses are 100% lethal for test animals while no significant disorders were observed at doses of 35 and 20 mg/kg. The biodistribution of the compound in organs and tissues was studied in mice with melanoma B-16. The maximum accumulation of labeled compound in tumor, skin, muscle, liver, kidneys, and spleen was observed 3 – 6 h after administration. A comparison of drug accumulation in tumor and normal tissues showed that the preparation does not possess pronounced tumor-targeting properties.
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The work was supported by a grant of the RFBR-BRFBR (X08P-065) (08-04-90025).
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 45, No. 12, pp. 15 – 18, December, 2011.
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Yadrovskaya, V.A., Koryakin, S.N., Ul’yanenko, S.E. et al. Synthesis, toxicity, and mouse biodistribution of 9-thiocyano-7,8-dicarba-nido-undecaborate during neutron-capture therapy. Pharm Chem J 45, 717–720 (2012). https://doi.org/10.1007/s11094-012-0709-0
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DOI: https://doi.org/10.1007/s11094-012-0709-0