从鬼臼毒素出发,通过简洁的合成路线合成了9个新型的鬼臼毒素五元氮杂环类衍生物,其结构经1H NMR,13C NMR,IR,HR-ESI-MS以及X单晶衍射确定.对合成的新化合物进行了体外抗肿瘤活性的筛选,结果表明,化合物10具有较好的细胞毒活性,IC50值为2.63~4.73μmol/L,对4种细胞株的活性均优于顺铂,可以作为先导化合物作进一步的结构修饰和更深入的活性研究. Starting from podophyllotoxin, nine novel podophyllotoxin five-membered azacyclic derivatives were synthesized by simple synthetic routes. Their structures were confirmed by 1H NMR, 13C NMR, IR, HR-ESI-MS and X-ray single crystal diffraction The results showed that compound 10 has good cytotoxic activity with IC50 value of 2.63 ~ 4.73μmol / L, and the activity of all the four cell lines was better than that of cis Platinum can be used as a lead compound for further structural modification and further activity studies.