DOMESTIC ANTITUMOR COMPOUND 2-[3-(2-CHLOROETHYL)-3-NITROSOUREIDO]-1,3- PROPANEDIOL (CHLONISOL). ACUTE TOXICITY

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Abstract

2-[3-(2-Chloroethyl)-3-nitrosoureido]-1,3-propanediol (Сhlonisol) is a representative of a separate group of derivatives of the class of nitrosoalkylureas – alkylnitrosoureidopropanediols, which are characterized by high antitumor activity on a wide range of experimental tumors. Chlonisol LD50 in male mice for intravenous administration was 35 mg/kg, intraperitoneal – 39 mg/kg, in female mice – 34 mg/kg and 36 mg/kg, respectively. In rats of males with intraperitoneal administration, LD50 was 30 mg/kg, in rats of females – 32 mg/kg. The maximum tolerated dose in mice, rats, guinea pigs and rabbits was 20 mg/kg. The tolerated dose for dogs was a dose of 2 mg/kg. Myelo-depression was a dose-limiting side effect. Lethal and sublethal doses of Chlonisol caused aplasia of the bone marrow and lymphoid organs, damage to the mucous membrane of the gastrointestinal tract, and dystrophic changes in the myocardium, lungs, liver, kidneys, pancreas, and reproductive organs. In the late stages after intraperitoneal administration of sublethal doses of Chlonisol, chylothorax and chyloperitoneum were found in some rats.

About the authors

A. N. Stukov

N.N. Petrov Scientifi c Research Center of Oncology, RF Ministry of Health

Author for correspondence.

Stukov Alexander Nikolaevich

197758, Saint Petersburg

Russian Federation

S. F. Vershinina

A.M. Granov Russian Research Center for Radiology and Surgical Technologies, RF Ministry of Health

Vershinina Sofia Fathutdinovna

197758, Saint Petersburg

Russian Federation

N. N. Kharitonova

S.M. Kirov Military Medical Academy

Email: natal56@mail.ru

Kharitonova Natalja Nicolaevna

194044, Saint Petersburg

Russian Federation

L. V. Filatova

N.N. Petrov Scientifi c Research Center of Oncology, RF Ministry of Health

Email: larisa_filatova@list.ru

Filatova Larisa Valentinovna

197758, Saint Petersburg

Russian Federation

D. Н. Latipova

N.N. Petrov Scientifi c Research Center of Oncology, RF Ministry of Health

Latipova Dilorom Hamidovna

197758, Saint Petersburg

Russian Federation

M. L. Tyndyk

N.N. Petrov Scientifi c Research Center of Oncology, RF Ministry of Health

Tyndyk Margarita Leonidovna

197758, Saint Petersburg

Russian Federation

Yu. G. Zmitrichenko

N.N. Petrov Scientifi c Research Center of Oncology, RF Ministry of Health

Email: zmitrichenko@gmail.com

Zmitrichenko Yuliya Gennadievna

197758, Saint Petersburg

Russian Federation

A. L. Semenov

N.N. Petrov Scientifi c Research Center of Oncology, RF Ministry of Health

Email: genesem7@mail.com

Semenov Alexander Leonidovich

197758, Saint Petersburg

Russian Federation

V. G. Bespalov

N.N. Petrov Scientifi c Research Center of Oncology, RF Ministry of Health

Email: bespalov_niio@mail.ru

Bespalov Vladimir Grigorievich

197758, Saint Petersburg

Russian Federation

T. Yu. Semiglazova

N.N. Petrov Scientifi c Research Center of Oncology, RF Ministry of Health

Semiglazova Tatiana Yuryevna

197758, Saint Petersburg

Russian Federation

References

  1. Kon’kov S.A., Stukov A.N., Reztsova V.V. etc. Alkylhydroperoxide and alkylatorspodophyllin – new group of anticancer compounds. Oncology Issues. 1998; 44 (1): 97-99 (in Russian).
  2. Ostrovskaya L.A, Filov V.A, Ivin B.A. et al. Chlonizol – the new alkylnitrosourea J drug with antitumor activity. Russian Biotherapeutic ournal. 1998; 3 (1): 37-48 (in Russian).
  3. Stukov A.N., Esikov K.A., Usmanova L.M. et al. Method of synthesis 2-[3-(2-chlorethyl)- 3-nitrosoureido]-1,3-propanediol owned with antitumor activity. Patent RF, № 2678846; 2018 (in Russian).
  4. Stukov A.N., Semiglasova T.Yu., Filatova L.V. et al. Use of the compound 2-[3-(2-chloroethyl)-3-nitrosoureido]-1,3- propanediol for the treatment of HER2- positive tumors in the experiment. Patent R F; № 2695787; 2018 (in Russian)

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Copyright (c) 2021 Stukov A.N., Vershinina S.F., Kharitonova N.N., Filatova L.V., Latipova D.Н., Tyndyk M.L., Zmitrichenko Y.G., Semenov A.L., Bespalov V.G., Semiglazova T.Y.


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