钯(Ⅱ)类抗肿瘤药物研究进展

Current development of Pd(Ⅱ) complexes as potential antitumor

20世纪60年代,美国密执安州立大学Rosenberg发现了顺铂具有抗癌活性,开辟了金属类抗肿瘤药物研究的新领域.经过40余年的研究,已相继成功开发了卡铂、奈达铂、奥沙利铂、舒铂、洛铂和双环铂等铂类抗肿瘤药物.虽然对于铂类抗肿瘤药物研究取得了一定的成绩,但在临床使用过程中也存在一些问题,如其毒副作用和抗药性,限制了其在临床上的进一步广泛应用.为了解决这些问题,科研工作者开始寻找新的金属类抗肿瘤药物以弥补现有铂类抗肿瘤药物的不足.在金属元素中,唯有钯(II)与铂(II)配合物具有相似或相同的结构特征,进而表现出相近或相似的化学性质.因此,继铂类抗肿瘤配合物后,钯(II)配合物作为潜在抗肿瘤药物成为一个诱人的领域.本文综述了近年来钯(II)类抗肿瘤药物的研究进展,并探讨了其构效关系,这对于指导新型钯(II)类抗肿瘤药物的合成具有重要的参考价值.

In 1960s, Rosenberg discovered the anticancer activity of cisplatin, and heralded a new era of anticancer drug research based on metallopharmaceuticals. During the past 40 years, carboplatin, nedaplatin, oxaliplatin, eptaplatin, lobaplatin and dicycloplatin have been successfully developed. Although some results were achieved for platinum anticancer drugs, some problems often limited their clinical use by severe toxic side-effects, as well as the intrinsic and acquired resistance possessed by various cancers. In order to solve these problems, new metal-based anticancer drugs were started to found. Based on the similarity of structural and chemical properties between platinum（II） and palladium（II） complexes, palladium（II） complexes as the potential antitumor drug have become an attractive field. This review summarized the current development of palladium（II） complexes as potential antitumor agents, and the structure-activity relationship were studied, which will be valuable for guiding the synthesis of new type palladium（II） anticancer drugs.