Abstract
The antitumor activity of 5-(5′,6′-benzocoumaro-3′-yl)methylaminouracil (BCMU) and its liposomal medicinal form was studied in comparison to 5-fluorouracil (5-FU), a well-known antitumor drug widely used in oncological practice. The half-lethal dose of BCMU is 14.8 ± 4.2 mg/kg, while the optimum effective dose of the drug is 6 mg/kg. In this dose, BCMU combines low toxicity with significant antitumor activity, which is manifested by increased tumor growth inhibition (TGI) at a 19% increase in the lifetime (LT) of experimental animals. The antitumor activity of the liposomal form of BCMU is quantitatively and qualitatively superior to that of the nonmodified compound and 5-FU, which is manifested by the most pronounced TGI value and by a significant LT increase.
Similar content being viewed by others
References
E. A. Parfenov and L. D Smirnov, Khim.-Farm. Zh., 22(12), 1438–1448 (1988).
Experimental Evaluation of Antitumor Drugs in USSR and USA [in Russian], Z. P. Sof’ina, A. B. Syrkin, A. Goldin, and K. Kleine (eds.), Meditsina, Moscow (1979).
I. V. Orlenko, S. N. Kovalenko, I. A Zhuravel’, et al., Fiziol. Aktiv. Rech., No. 3, 25–28 (2001).
V. G. Budker, T. E. Vakhrusheva, E. V. Keseleva, and N. B. Khristolyubova, Khim.-Farm. Zh., 21(1), 347–352 (1987).
Author information
Authors and Affiliations
Additional information
__________
Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 40, No. 6, pp. 6–7, June, 2006.
Rights and permissions
About this article
Cite this article
Marchenko, M.M., Kopyl’chuk, G.P., Shmarakov, I.A. et al. Synthesis and antitumor activity of 5-(5′,6′-benzocoumaro-3′-yl)methylaminouracil hydrobromide and its liposomal medicinal form. Pharm Chem J 40, 296–297 (2006). https://doi.org/10.1007/s11094-006-0113-8
Received:
Issue Date:
DOI: https://doi.org/10.1007/s11094-006-0113-8