Sosnovsky G, Rao N U
Cancer Lett. 1985 Dec;29(3):309-22. doi: 10.1016/0304-3835(85)90142-9.
The scope of the structure-anticancer activity relationship among various aliphatic and aromatic hydrazones containing the N,N,N',N'-bis(1,2-ethanediyl)-phosphoric diamide moiety was studied. A total of 19 compounds were tested in vivo, using murine lymphocytic leukemia P388. At optimum dose all these compounds were active. The highest activity was exhibited by the N,N;N',N'-bis(1,2-ethanediyl)-[N2-(p-chlorobenzylidene)-N1- hydrazin-1-yl]phosphoric triamide, N,N;N',N'-bis(1,2-ethanediyl)-N2-(p-chlorobenzylidene)-N1- methylhydrazin-1-yl]phosphoric triamide and N,N;N',N'-bis(1,2-ethanediyl)-[N2-(p-chlorobenzylidene)-N1- phenylhydrazin-1-yl]phosphoric triamide as is evidenced by the percent T/C of 212, 194 and 192, respectively. An attempt was made to correlate the anticancer activities with the corresponding lipophilicities. On the basis of the activity-lipophilicity results, it is concluded that, in general, the activity scale follows the lipophilicity scale in the reverse order, i.e. the more active compounds possess lower lipophilicity than the less active compounds.
研究了含N,N,N',N'-双(1,2-乙二基)-磷酸二酰胺部分的各种脂肪族和芳香族腙的结构-抗癌活性关系范围。使用小鼠淋巴细胞白血病P388对总共19种化合物进行了体内测试。在最佳剂量下，所有这些化合物均具有活性。N,N;N',N'-双(1,2-乙二基)-[N2-(对氯亚苄基)-N1-肼基-1-基]磷酸三酰胺、N,N;N',N'-双(1,2-乙二基)-N2-(对氯亚苄基)-N1-甲基肼基-1-基]磷酸三酰胺和N,N;N',N'-双(1,2-乙二基)-[N2-(对氯亚苄基)-N1-苯基肼基-1-基]磷酸三酰胺表现出最高活性，其T/C百分比分别为212、194和192。尝试将抗癌活性与相应的亲脂性相关联。根据活性-亲脂性结果得出结论，一般来说，活性顺序与亲脂性顺序相反，即活性较高的化合物比活性较低的化合物具有更低的亲脂性。
