Keppler B K, Michels K
Arzneimittelforschung. 1985;35(12):1837-9.
Ten six-coordinate dihalogenobis (1.3-diketonato)zirconium (IV) and hafnium (IV) complexes as well as seven halogenotris(1.3-diketonato) zirconium(IV) and hafnium(IV) species were prepared and characterized by their elemental analysis, IR- and NMR-spectra. Their antitumor activity was tested using the intraperitoneally transplanted Sarcoma 180 tumor system in mice. Cisplatin was used in several doses as positive control compound. Seven complexes were highly active. The ratio of median survival time of treated to untreated control animals ranged up to 3 (T/C = 300%; the experiment was interrupted after that time) for these compounds. Significance according to Kruskal-Wallis test, long-time survivors, and animals which are dead on day 5 and day 30 are given. The possible mechanism of action compared to cisplatin is discussed.
制备了十种六配位二卤代双(1,3 - 二酮基)锆(IV)和铪(IV)配合物以及七种卤代三(1,3 - 二酮基)锆(IV)和铪(IV)物种,并通过元素分析、红外光谱和核磁共振光谱对其进行了表征。使用小鼠腹腔移植肉瘤180肿瘤系统测试了它们的抗肿瘤活性。顺铂以几种剂量用作阳性对照化合物。七种配合物具有高活性。对于这些化合物,治疗组与未治疗对照组动物的中位生存时间之比高达3(T/C = 300%;此后实验中断)。给出了根据克鲁斯卡尔 - 沃利斯检验的显著性、长期存活者以及在第5天和第30天死亡的动物情况。讨论了与顺铂相比可能的作用机制。