Abstract: Ten ursolic acid derivatives were designed from the lead compound ursolic acid by introducing 1, 2, 3-triazole at C-3 and C-28. The target compounds were synthesized and characterized by ¹H NMR and ¹³C NMR. MTT assay was used to study the antitumor activity of these compounds in human cancer cells with high expression (MCF-7 and SGC-7901). The results showed that the antitumor activity of all compounds on MCF-7 and SGC-7901 tumor cells was significantly higher than that of ursolic acid. The compound Ⅱ₄ exhibited significant antitumor activity which was equivalent to the positive control drug nilotinib, molecular docking showed that the compound Ⅱ₄ have high binding ability with c-Kit, which deserves further research.