鬼臼毒素衍生物的研究进展

Recent studies on podophyllotoxin derivatives

目的对鬼臼毒素衍生物的研究概况进行综述,为鬼臼毒素衍生物的深入研究提供依据。方法通过阅读近5年来29篇相关文献报道,从鬼臼毒素衍生物的抗癌作用机制、合成、构效关系等方面对其目前的研究概况进行综述。结果鬼臼毒素衍生物的合成目前仍以鬼臼毒素C4位修饰为主,最新的文献研究表明与C4位有含氧取代基的鬼臼毒素衍生物相比,相应位置没有取代基的鬼臼毒素类似物细胞毒活性更强。结论为鬼臼毒素衍生物的合成提供参考数据。

Objective To review the researches on the podophyllotoxin derivatives, and provide the basis for its further research. Methods Papers published mainly in the recent 5 years had been reviewed including anticancer mechanism, synthesis and structure-activity relationship. Results Most of research efforts have been focused on exploring different 4-substituted podophyllotoxin analogues. Podophyllotoxin analogues with 4 oxygenated group exhibited significantly lower cytotoxic activity than corresponding analogues without 4-substitution. Conclusions This review provides a useful reference for the synthesis of podophyllotoxin derivatives.