Zeller W J, Schreiber J, Ho A D, Schmähl D, Eisenbrand G
J Cancer Res Clin Oncol. 1984;108(1):164-8. doi: 10.1007/BF00390991.
First investigations on the therapeutic activity of a new group of steroid-linked N-(2-chloroethyl)-N-nitrosocarbamoyl-L-alanine esters (CNC-L-alanine esters) in a nitrosourea-sensitive rat leukemia (L 5222) characterized by a relatively high content of glucocorticoid binding sites are presented. Despite a considerable range of optimal and toxic doses of the different analogs, the respective therapeutic ratios do not appear to be significantly influenced by the nature of the carrier molecules to which CNC-L-alanine is attached. However several steroid-linked representatives are distinctly more active than CNC-L-alanine. The androsterone-3-ester and the dihydrotestosterone-17-ester, in particular effected high percentages of cures in contrast to CNC-L-alanine.
首次对一组新的与甾体相连的N-(2-氯乙基)-N-亚硝基氨基甲酰-L-丙氨酸酯(CNC-L-丙氨酸酯)在一种对亚硝基脲敏感的大鼠白血病(L 5222)中的治疗活性进行了研究,该白血病的糖皮质激素结合位点含量相对较高。尽管不同类似物的最佳剂量和毒性剂量范围相当大,但各自的治疗比率似乎并未受到与CNC-L-丙氨酸相连的载体分子性质的显著影响。然而,几种与甾体相连的代表物明显比CNC-L-丙氨酸更具活性。尤其是雄甾酮-3-酯和双氢睾酮-17-酯,与CNC-L-丙氨酸相比,实现了高治愈率。