CNC-氨基酸和-寡肽的新衍生物：实验性抗肿瘤活性。
New derivatives of CNC-amino acids and -oligopeptides: experimental antitumor activity.
作者信息
Zeller W J
出版信息
J Cancer Res Clin Oncol. 1986;111(2):154-6. doi: 10.1007/BF00400755.
Abstract
The experimental antitumor activity of a series of new nitrosoureas is described in which the chloroethylnitrosocarbamoyl (CNC) group is attached to different carrier molecules: amino acids and oligopeptides. Of a group of 10 CNC-amino acid amide derivatives the majority displayed high therapeutic activity in L 5222 leukemia. Some compounds, especially the proline and sarcosine derivatives, showed favorable therapeutic ratios; 12 CNC-oligopeptides displayed a more or less pronounced therapeutic activity in L 1210 leukemia. Compounds bearing a free carboxy group were less active than the corresponding unsubstituted or N-methyl substituted amides.
摘要
本文描述了一系列新型亚硝基脲的实验抗肿瘤活性，其中氯乙基亚硝基甲酰基（CNC）基团连接到不同的载体分子上：氨基酸和寡肽。在一组10种CNC-氨基酸酰胺衍生物中，大多数在L 5222白血病中表现出高治疗活性。一些化合物，特别是脯氨酸和肌氨酸衍生物，显示出良好的治疗比率；12种CNC-寡肽在L 1210白血病中表现出或多或少明显的治疗活性。带有游离羧基的化合物比相应的未取代或N-甲基取代的酰胺活性更低。
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3
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4
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