Köpf-Maier P, Klapötke T
Institut für Anatomie, Freie Universität Berlin.
Cancer Chemother Pharmacol. 1992;29(5):361-6. doi: 10.1007/BF00686004.
The antitumor activity of the three air-stable bis(cyclopentadienyl)rhenium derivatives [(C5H5)2-ReCl2]+Cl-,[(C5H5)2ReCl2]+[AsF6]- , and [(C5H5)2-ReCl2]+[SbF6]- was tested against Ehrlich ascites tumor in female CF1 mice. All three compounds contain the group-7 transition metal rhenium in the +5 oxidation state as their central metal atom. They are ionic, salt-like complexes that are composed of the cationic [(C5H5)2ReCl2]+ moiety and one of the negatively charged counterions Cl-, AsF6-, or SbF6-. Both the chloro and the hexafluoroarsenate complexes induced a maximal cure rate of 100% when given either in a dose range of 120-160 mg/kg (rhenocene trichloride) or at a single dose of 180 mg/kg (hexafluoroarsenate derivative). The hexafluoroantimonate complex effected a maximal cure rate of only 50% at 60 mg/kg. For the two former compounds, the values for the therapeutic index (TI) amounted to 1.7 and 2.1, respectively. No impairment of the general condition or pathologic symptoms in the viscera could be detected by observation of the animals during the days following treatment with therapeutic doses or by autopsy of the surviving animals on the key date (day 90). The rhenocene derivatives investigated in the present study represent a new class of antitumor metallocene compounds as well as the first rhenium(V) complexes exerting cytostatic activity.
测试了三种空气稳定的双（环戊二烯基）铼衍生物[（C5H5）2-ReCl2]+Cl-、[（C5H5）2ReCl2]+[AsF6]-和[（C5H5）2-ReCl2]+[SbF6]-对雌性CF1小鼠艾氏腹水瘤的抗肿瘤活性。这三种化合物均以处于+5氧化态的第7族过渡金属铼作为其中心金属原子。它们是离子型的类盐配合物，由阳离子[（C5H5）2ReCl2]+部分和带负电荷的抗衡离子Cl-、AsF6-或SbF6-之一组成。氯配合物和六氟砷酸盐配合物在120 - 160 mg/kg剂量范围内（二氯茂铼）或单次剂量180 mg/kg（六氟砷酸盐衍生物）给药时，诱导的最大治愈率均为100%。六氟锑酸盐配合物在60 mg/kg时的最大治愈率仅为50%。对于前两种化合物，治疗指数（TI）值分别为1.7和2.1。在给予治疗剂量后的几天内观察动物，或在关键日期（第90天）对存活动物进行尸检，均未发现一般状况受损或内脏出现病理症状。本研究中研究的二氯茂铼衍生物代表了一类新型的抗肿瘤茂金属化合物，也是首批具有细胞抑制活性的铼（V）配合物。
