Synthesis and Anti-tumor Activity of Ursolic Acid C-28 Tetrazole Derivatives

Abstract: Thirteen novel ursolic acid derivatives were synthesized by structurally modifying the C-3 and C-28 positions of ursolic acid (as the parent structure) with the introduction of tetrazole active fragments. The target compounds are synthesized and characterized by 1H NMR and 13C NMR. The in vitro anti-tumor activity of the compounds was preliminarily screened using human cancer cells with high expression (breast cancer MCF-7 and gastric cancer SGC-7901 cells) by the MTT method. The results showed that all compounds exhibited significantly higher inhibitory activity against MCF- 7 and SGC-7901 tumor cells than ursolic acid. Among them, compound 8 demonstrated potent antitumor activity against both cell lines, with efficacy similar to the positive control nilotinib. Molecular docking indicated its high affinity for c-Kit, making it worthy of further research.