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N-[N'-(2-氯乙基)-N'-亚硝基氨基甲酰基]-氨基酸酯和酰胺的抗肿瘤活性

Antineoplastic activity of esters and amides of N-[N'-(2-chloroethyl)-N'-nitrosocarbamoyl]-aminoacids.

作者信息

Zeller W J, Ehresmann K, Eisenbrand G

出版信息

J Cancer Res Clin Oncol. 1984;108(2):249-51. doi: 10.1007/BF00402478.

Abstract

The antineoplastic activity of 7 ester derivatives and 15 amide derivatives of N-[N'-(2-chloroethyl)-N'-nitrosocarbamoyl (CNC)]-aminoacids was examined in transplanted rat leukemia L 5222. All esters except the ethylester of CNC-L-isoleucine showed only a moderate antitumor activity. CNC-L-isoleucine ethylester effected some cures and showed the lowest toxicity of this series of compounds. The amide derivatives on the other hand were highly active in L 5222; all compounds effected cures in the dose range investigated.

摘要

研究了N-[N'-(2-氯乙基)-N'-亚硝基氨基甲酰基(CNC)]-氨基酸的7种酯衍生物和15种酰胺衍生物对移植性大鼠白血病L 5222的抗肿瘤活性。除CNC-L-异亮氨酸乙酯外,所有酯仅表现出中等抗肿瘤活性。CNC-L-异亮氨酸乙酯实现了部分治愈,且是该系列化合物中毒性最低的。另一方面,酰胺衍生物对L 5222具有高活性;在所研究的剂量范围内,所有化合物都实现了治愈。

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