高水溶性铂类抗肿瘤药物的设计与合成

摘要

目的 设计与合成具有高水溶性的铂类抗肿瘤药物.方法 通过在丙二酸铂结构中偶联糖分子设计出目标化合物并合成取得水溶性抗肿瘤药物.结果 得到了迄今水溶性最好的金属铂类抗肿瘤化合物,其动物模型抗肿瘤活性和安全性均优于顺铂和卡铂.结论 通过糖分子偶联设计取得的新型铂类抗肿瘤药物能够解决一般铂类药物的低水溶性问题.经初步动物模型抗肿瘤药效实验证明该类药物具有理想的抗肿瘤效果.%Objective To design and synthesize Platinum antineoplastic drugs with high water solubility. Methods Sugar molecular was coupled to the malonic acid Platinum structure to design and synthesize Platinum antineoplastic drugs with high water solubility. Results Metal Platinum antineoplastic compound with best water-solubility was produced, and its antineoplastic activity and safety were better than those of Cisplatin and Carboplatin on animal model. Conclusion Neotype Platinum antineoplastic drug, which is produced through the sugar molecule coupling design, can solve low water-solubility problem of general Platinum drugs. Preliminary antineoplastic efficacy experiment on animal model demonstrates that this kind of medicine has ideal antineoplastic effect.