Braun R, Hefter E
Arzneimittelforschung. 1977;27(11):2114-7.
The inhibition of uridine and thymidine in Ehrlich ascites cells is a basic property of the methylhydrazone structure and is reinforced by introducing a beta-chloroethyl group. This was shown by variation of the substituents at the N'-nitrogen atom of N'-methyl-N'-beta-chloroethyl-benzaldehyde hydrazone. Probably this action is due to an ethylenimmonium intermediate. This is derived from the observation that substituents which increase the nucleophilic property of the N'-nitrogen atom show a greater inhibitory effect in vitro. The therapeutic effect, however, is not enhanced when tested on the solid Ehrlich ascites tumor of mice. A better therapeutic effect resulted from introduction of chlorine atoms in positions 3 and 4 of the ring which inhbiits as well a probable metabolic hydroxylation of the ring.
对艾氏腹水癌细胞中尿苷和胸苷的抑制作用是腙结构的基本特性，引入β-氯乙基可增强这种作用。这是通过改变N'-甲基-N'-β-氯乙基苯甲醛腙的N'-氮原子上的取代基来证明的。这种作用可能是由于乙烯亚铵中间体引起的。这是基于这样的观察结果：增加N'-氮原子亲核性的取代基在体外表现出更大的抑制作用。然而，在小鼠实体艾氏腹水瘤上进行测试时，治疗效果并未增强。在环的3位和4位引入氯原子会产生更好的治疗效果，这也抑制了环可能的代谢羟基化。
