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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.

DOI:10.1007/BF00402478
PMID:6470033
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12253009/
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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1
Antineoplastic activity of esters and amides of N-[N'-(2-chloroethyl)-N'-nitrosocarbamoyl]-aminoacids.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
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引用本文的文献

1
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2
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Br J Cancer. 1986 Jul;54(1):137-98. doi: 10.1038/bjc.1986.164.
3
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Br J Cancer. 1989 Mar;59(3):335-40. doi: 10.1038/bjc.1989.66.

本文引用的文献

1
Examination of newly synthesized 2-chloroethyl-nitrosoureas on rat leukemia L 5222.新型合成的2-氯乙基亚硝基脲对大鼠白血病L 5222的研究。
Oncology. 1981;38(1):39-42. doi: 10.1159/000225519.
2
Chemotherapeutic activity of 2-chloroethylnitrosocarbamoyl derivatives of amino acids in a transplanted rat leukemia (L 5222).氨基酸的2-氯乙基亚硝基氨基甲酰衍生物对移植大鼠白血病(L 5222)的化疗活性
Arzneimittelforschung. 1982;32(5):484-6.
3
(2-Chloroethyl)nitrosourea congeners of amino acid amides.氨基酸酰胺的(2-氯乙基)亚硝基脲类似物。
J Med Chem. 1982 Jul;25(7):829-32. doi: 10.1021/jm00349a012.
4
Chemotherapeutic activity of new 2-chloroethylnitrosoureas in rat L5222 leukemia: comparison of bifunctional and water-soluble derivatives with 1,3-bis(2-chloroethyl)-1-nitrosourea.
J Natl Cancer Inst. 1978 Feb;60(2):345-8. doi: 10.1093/jnci/60.2.345.
5
Examination of four newly synthesized 2-chloroethylnitrosoureas in comparison with BCNU, CCNU, MeCCNU, chlorozotocin and hydroxyethyl-CNU in preterminal rat leukemia L 5222.将四种新合成的2-氯乙基亚硝脲与卡莫司汀、洛莫司汀、司莫司汀、链脲佐菌素和羟乙基亚硝脲在晚期大鼠白血病L 5222中进行比较研究。
J Cancer Res Clin Oncol. 1979 Sep;95(1):43-9. doi: 10.1007/BF00411108.