玫瑰树碱(ellipticine)是一种来源于天然产物的细胞毒生物碱,具有抗肿瘤作用和抗艾滋病毒活性。自1959年首次被分离后,众多合成化学家设计并完成了玫瑰树碱的全合成路线。本文根据起始原料的不同对玫瑰树碱及衍生物的合成方法进行了综述,同时探讨了该类化合物的抗肿瘤活性作用机制,还对玫瑰树碱的抗肿瘤的构效关系进行了总结。 Ellipticine is a cytotoxic alkaloid derived from natural products that has anti-tumor effects and anti-HIV activity. Since being first isolated in 1959, many synthetic chemists have designed and completed the fully synthetic route of ellipticine. In this paper, the synthetic methods of ellipticine and its derivatives were reviewed according to the different starting materials. The antitumor activity mechanism of these compounds was also discussed. The antitumor activity-activity relationship of ellipticine was also summarized.