Abstract: Rocaglamide and its analogues are extracted from the genus of Melia L. Most of them have insecticidal,anti-inflammatory and anticancer activities due to their unique chemical structure. At present, it has been found that rocaglamides have the effect of inducing apoptosis in lung cancer, renal cell carcinoma, pancreatic cancer, and malignant peripheral nerve sheath tumor, but have no toxic effects on normal cells. The anti-tumor mechanism of rocaglamides mainly includes: inhibiting the initiation of translation of cancer cells, regulating cell cycle, inducing apoptosis of tumor cells, inhibiting cell proliferation, and reducing drug cytotoxicity. Therefore, rocaglamide and its analogues as potential anticancer drugs have shown great application potential, and relative researches have been paid more attentions in recent years. In this review, the discovery progress, structural characteristics, anticancer activity and mechanisms of activity in cancer involved in the secondary metabolite of plants of the genus of Melia L. were summarized. In order to provide theoretical basis and research ideas for the further research and development of rocaglamides, the application prospects of rocaglamides were prospected.