Schmidt H, Liss E
Arzneimittelforschung. 1978;28(11):2150-2.
Considerable quantitative differences have been observed between alkylating agents with respect to their effect on cell multiplication of tumor cells. The ethyleneimine derivative triaziquone is approximately a thousand times more effective than the biologically active conversion products of the nitrogen mustard derivative cyclophosphamide. The main difference may be directly related to the extent to which each of the two substances is able to pass into the cells. After a 60-min incubation period approximately 1% of the cyclophosphamide conversion products have been bound by ascites tumor cells. The uptake of the more lipophilic triaziquone, however, is nearly 50% under identical conditions.
关于烷化剂对肿瘤细胞增殖的影响，已观察到相当大的定量差异。乙烯亚胺衍生物三嗪醌的效力约为氮芥衍生物环磷酰胺生物活性转化产物的一千倍。主要差异可能直接与这两种物质各自进入细胞的程度有关。孵育60分钟后，约1%的环磷酰胺转化产物已被腹水肿瘤细胞结合。然而，在相同条件下，亲脂性更强的三嗪醌的摄取率接近50%。
