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Synthesis and Antitumor Activity of 2-[3-(2-Chloroethyl)-3-Nitrosoureido]-1,3-Propanediol (Chlonisol)
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2020-09-01 , DOI: 10.1007/s11094-020-02242-7
A. N. Stukov , K. A. Esikov , L. M. Usmanova , N. N. Kharitonova , S. F. Vershinina , Yu. G. Zmitrichenko , L. V. Filatova , D. Kh. Latipova , A. L. Semenov , V. G. Bespalov , T. Yu. Semiglazova

The reaction of 2-chloroethylisocyanate and 2-amino-1,3-propanediol in MeCN–MeOH yielded 2-[3-(2-chloroethyl) ureido]-1,3-propanediol, which was nitrosated using sodium nitrite in 50% formic acid to obtain 2-[3-(2-chloroethyl)-3-nitrosoureido]-1,3-propanediol (chlonisol). A single administration of chlonisol at a non-toxic dose of 15 mg/kg increased by 170% the median life expectancy of mice with P-388 leukemia and cured 100% of rats with Walker 256 carcinosarcoma.

中文翻译:

2-[3-(2-Chloroethyl)-3-Nitrosoureido]-1,3-Propanediol (Chlonisol) 的合成和抗肿瘤活性

2-氯乙基异氰酸酯和 2-氨基-1,3-丙二醇在 MeCN-MeOH 中反应生成 2-[3-(2-氯乙基) 脲基]-1,3-丙二醇,使用 50% 甲酸亚硝酸钠将其亚硝化酸得到 2-[3-(2-氯乙基)-3-亚硝基脲]-1,3-丙二醇(氯苯​​甲醚)。以 15 mg/kg 的无毒剂量单次给药氯苯甲醚可使患有 P-388 白血病的小鼠的平均预期寿命增加 170%,并治愈了 100% 患有 Walker 256 癌肉瘤的大鼠。
更新日期:2020-09-01
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