Giraldi T, Houghton P J, Taylor D M, Nisi C
Cancer Treat Rep. 1978 May;62(5):721-5.
Two dimethyltriazenoimidazoles, DTIC and BRL 51308, and a benzenoid dimethyltriazene, CB 10286, have been examined for their effects in mice bearing Lewis lung carcinoma. A slight reduction of primary tumor growth was found after treatment with DTIC and BRL 51308, whereas CB 10286 caused no significant effect. On the contrary, all the tested compounds sharply reduced the number of lung metastases and also resulted in a high proportion of animals free of metastases at death. No significant cytotoxic effect of the triazenes was observed in small established pulmonary tumors, as determined by evaluating the effects of treatment on the fractional incorporation of 3H-TdR into DNA of the lung colonies. These results are in contrast to those obtained with a purely cytotoxic agent, cyclophosphamide, and indicate that all three triazene derivatives tested have selective antimetastatic properties.
研究了两种二甲基三氮烯咪唑(达卡巴嗪和BRL 51308)以及一种苯类二甲基三氮烯(CB 10286)对携带Lewis肺癌的小鼠的影响。用达卡巴嗪和BRL 51308治疗后,发现原发性肿瘤生长略有减少,而CB 10286没有显著效果。相反,所有测试化合物都显著减少了肺转移瘤的数量,并且导致很大比例的动物在死亡时没有转移瘤。通过评估治疗对3H-TdR掺入肺集落DNA的分数的影响来确定,在已形成的小肺肿瘤中未观察到三氮烯的显著细胞毒性作用。这些结果与用纯细胞毒性药物环磷酰胺获得的结果相反,表明所测试的所有三种三氮烯衍生物都具有选择性抗转移特性。