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合成了一个新的抗肿瘤铂(Ⅱ)络合物—二氨去甲基斑蝥酸根合铂(Ⅱ),以IR、EXAFS研究鉴定其结构,与元素分析一致。此络合物中,去甲基斑蝥酸的两个羧基与铂配位。用EC细胞及荷瘤小鼠进行药理实验,并与cis-DDP及秋水仙碱对照,显示其抗肿瘤活性远高于秋水仙碱,略低于cis—DDP。LD_(50)约为cis-DDP的4倍。
A new anti-tumor platinum (Ⅱ) complex, diammine demethyl cantharidate platinum (Ⅱ) was synthesized and its structure was identified by IR and EXAFS. It was consistent with the elemental analysis. In this complex, the two carboxyl groups of desmethylcantharidine are coordinated to platinum. Pharmacological experiments with EC cells and tumor-bearing mice and cis-DDP and colchicine control showed that its anti-tumor activity is much higher than colchicine, slightly lower than cis-DDP. LD_ (50) is about 4 times cis-DDP.