The invention discloses tylophora ovata base analogs with anti-tumor activity and a preparation method and a use thereof. The tylophora ovata base analogs can be applied in the preparation of drugs for treating malignant tumors, leukemia and cancers, and the compound structural formula is as follows: R1, R2, R3 or R4 can be CH3O, R1R2, R3R4 and OCH2O, and R1, R2, R3 and R4 can not be CH3O at the same time. The tylophora ovata base analogs have the characteristics of high efficiency, low toxicity and significant role of inhibiting tumor cells, and can be applied in anti-cancer new drugs; the tylophora ovata base analogs are synthesized by adopting the one kettle way, the process is not separated, and final products are separated; and PIDA is added for synthesis, the synthesis route is simple, the efficiency is high and the cost is low.