Eisenbrand G, Fiebig H H, Zeller W J
Z Krebsforsch Klin Onkol Cancer Res Clin Oncol. 1976 Aug 30;86(3):279-86. doi: 10.1007/BF00286946.
The synthesis of new analogs of the anticancer agent BCNU is described. It involves the preparation of N-(2-chloroethyl)-N-nitrosocarbamoylazide and its reaction with aliphatic diamines and aminoalcohols to yield 1,1'-polymethylenebis 3-(2-chloroethyl)-3-nitrosoureas and 1-(omega-hydroxyalkyl)-3-(2-chloroethyl-3-nitrosoureas. Screening for chemotherapeutic activities of the newly synthesized nitrosoureas against rat leukemia L 5222 and s.c. Walker carcinosarcoma 256 revealed remarkable differences between individual compounds. The water soluble 1-(2-hydroxyethyl)-3-(2-chloroethyl)-3-nitrousourea was the most active compound of this series, effecting 90% cures in i.p. inoculated L5222 leukemia.
本文描述了抗癌药物卡莫司汀新类似物的合成。该合成过程包括制备N-(2-氯乙基)-N-亚硝基氨基甲酰叠氮，并使其与脂肪族二胺和氨基醇反应，生成1,1'-聚亚甲基双-3-(2-氯乙基)-3-亚硝基脲和1-(ω-羟烷基)-3-(2-氯乙基)-3-亚硝基脲。对新合成的亚硝基脲针对大鼠白血病L5222和皮下接种的沃克癌肉瘤256的化疗活性进行筛选，结果显示各化合物之间存在显著差异。水溶性的1-(2-羟乙基)-3-(2-氯乙基)-3-亚硝基脲是该系列中活性最高的化合物，对腹腔接种的L5222白血病的治愈率达90%。
