肿瘤的化学治疗——ⅩⅩⅥ.胺羧类金属络合物抗癌作用的研究

化合物Ⅰ及Ⅱ为氨三乙酸(NTA)的类似物,其中一或三个羧甲基分别换以β-巯基乙基,与若干过渡元素及锑或砷所形成的金属衍生物,其比例为1:1.相当于集二分子EDTA于一体的Ⅲ,不与亚锑酸作用,与若干过渡元素所形成的比例为一分子络合剂与二原子金属.上述金属衍生物供动物肿瘤试验,初步报告,Ⅱ-As、Ⅲ-Cu及Ⅲ-Co对肉瘤180稍有抑制作用。

TUMOUR CHEMOTHERAPY ⅩⅩⅥ. STUDIES ON ANTITUMOUR ACTIVITIES OF METAL COMPLEXES OF AMINOCARBOXYLIC ACIDS

Comparative analyses have established correlations between the amount of certain trace metals in human organs and the frequency of cancer, and the role of metals in the function of many enzymes has been well documented. Therefore, attention is drawn to the general importance of the distribution of these elements in normal and tumour tissues. A number of metals are concerned in the causation of cancer while others are connected with the antitumour activities. From the evidence accumulated in the literature, it is shown that various elements, particularly the first row of the transition elements in the periodic chart, are capable of exerting either effects. We have therefore prepared the transition metal complexes related to ethylene- diaminetetraacetic acid and nitrilotriacetic acid whose antimonial chelates have been given clinical trial as antitumour agents. Either ⅠorⅡ, on treatment with metal acetate or metal chloride, gave the corresponding metal complexes by the mole ratio of 1 : 1. The corresponding metal complexes of Ⅲ were similarly prepared. In such complex salts one mole of chelating agent combined with two metal atoms. Preliminary pharmacological tests revealed that Ⅱ-As, Ⅲ-Cu, Ⅲ-Co produced a slight inhibition on the growth of sarcoma 180.