Schmid J R, Fiebig H H, Eisenbrand G, Löhr G W
J Cancer Res Clin Oncol. 1986;111(1):31-4. doi: 10.1007/BF00402772.
A total of 11 newly synthesized 2-chloroethyl-nitrosoureas and 1 2-fluoroethyl-nitrosourea with short-chain substituents were tested for their cytostatic activity on the L1210 mouse leukemia in comparison to clinically used nitrosoureas. Initial experiments showed advantages of the i.v. route for tumor inoculation. Therefore, the anatomical generalisation of tumor cells after i.v. injection was studied by bio-assay. Tumor cell determinations in different organs were 10 to 100 times higher compared with i.p. implantation. Of the new compounds 10 showed marked cytostatic activity in this tumor model by producing cures, and 5 of them must be considered as superior to BCNU, the most commonly used nitrosourea.
总共测试了11种新合成的带有短链取代基的2-氯乙基亚硝基脲和1种2-氟乙基亚硝基脲对L1210小鼠白血病的细胞生长抑制活性,并与临床使用的亚硝基脲进行了比较。初步实验显示静脉注射途径用于肿瘤接种具有优势。因此,通过生物测定法研究了静脉注射后肿瘤细胞在解剖学上的扩散情况。与腹腔注射相比,不同器官中的肿瘤细胞测定值高出10到100倍。在这个肿瘤模型中,10种新化合物通过产生治愈效果表现出显著的细胞生长抑制活性,其中5种必须被认为优于最常用的亚硝基脲——卡莫司汀(BCNU)。