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在寻找新型抗癌药物的过程中。26. 几种替派、硫替派、硒替派和氮杂环丁烷类似物（包括含有氨氧基部分的同系物）的抗癌活性比较。

In the search for new anticancer drugs. 26. A comparison of anticancer activities of several TEPA, thio-TEPA, Seleno-TEPA, and azetidine analogs, including congeners containing an aminoxyl moiety.

作者信息

Sosnovsky G, Lukszo J, Konieczny M, Purgstaller K, Laib F

机构信息

Department of Chemistry, University of Wisconsin, Milwaukee 53201.

出版信息

J Pharm Sci. 1994 Jul;83(7):982-8. doi: 10.1002/jps.2600830713.

DOI:10.1002/jps.2600830713
PMID:7525922
Abstract

A series of TEPA, Thio-TEPA, Seleno-TEPA, and azetidine analogs, including congeners containing an aminoxyl moiety, were synthesized and evaluated in vivo for anticancer activity against the murine lymphocytic leukemia P388. All aziridine derivatives were found to be active with an increase in life span ranging from 42% to 272%, and all azetidine analogs were rated as inactive with one marginal exception. An attempt was made to rationalize the results on the basis of the lipophilic properties of the compounds. The most active compound (8) possessed the most balanced lipophilic properties, corresponding to a log P value near zero.

摘要

合成了一系列的三乙烯磷酰胺（TEPA）、硫代三乙烯磷酰胺（Thio - TEPA）、硒代三乙烯磷酰胺（Seleno - TEPA）以及氮杂环丁烷类似物，包括含有氨氧基部分的同系物，并在体内对其抗小鼠淋巴细胞白血病P388的活性进行了评估。发现所有氮丙啶衍生物均具有活性，寿命延长范围为42%至272%，并且除了一个边缘例外，所有氮杂环丁烷类似物均被评定为无活性。尝试根据化合物的亲脂性对结果进行合理说明。活性最高的化合物（8）具有最平衡的亲脂性，对应于接近零的log P值。

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