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目的寻求高效低毒的新一代铂类抗肿瘤药物。方法以六氯合铂 (Ⅳ )酸钾 (K2 PtCl6)为原料 ,设计合成了一系列顺铂 (cisplatin)类似物 ,将其依次氧化、酰化 ,合成了 11个新型铂 (Ⅳ )类配合物 ,结构通式为 :PtCl2 (OR1) 2 (NH2 R) 2 。并以溴化乙锭 (Etd)为荧光探针 ,通过配合物与DNA相互作用而引起体系的荧光变化 ,测定最大荧光淬灭百分率 (Rm) ,计算结合常数Km ,由此推测配合物抗癌活性。结果所合成铂 (Ⅳ )配合物的化学结构由元素分析和光谱分析所证实 ,其中 7个化合物 (6c～ 6e ,7c～7f)尚未见文献报道。试验测得受试配合物Rm值和Km计算值均较顺铂低 ,其活性顺序为 :顺铂 >6a >6c>6d。结论铂 (Ⅳ )配合物是一类具有重要研究价值和开发前景的抗肿瘤剂。
Objective To seek a new generation of platinum anti-tumor drugs with high efficiency and low toxicity. Methods A series of analogs of cisplatin were designed and synthesized using K2 PtCl6 as raw material, which were sequentially oxidized and acylated to synthesize 11 novel platinum (Ⅳ) complexes Objects, the general structure is: PtCl2 (OR1) 2 (NH2 R) 2. (Etd) was used as fluorescent probe, the fluorescence of the system was induced by the interaction between the complex and DNA, the maximum fluorescence quenching percentage (Rm) was determined, and the binding constant Km was calculated. active. Results The chemical structure of the synthesized platinum (Ⅳ) complex was confirmed by elemental analysis and spectroscopic analysis. Seven compounds (6c ~ 6e, 7c ~ 7f) have not been reported in the literature. The measured values of Rm and Km of the tested compounds were lower than that of cisplatin. The order of activity was cisplatin> 6a> 6c> 6d. Conclusion Platinum (Ⅳ) complexes are a class of antitumor agents with important research value and development prospects.