Abstract: Twelve derivatives of asiatic acid were synthesized through acylation, alkylation, oxidative dehydrogenation and other reactions using asiatic acid from usoxane-type pentacyclic triterpenoids as the parent compound. Their structures were confirmed by ¹H NMR and ¹³C NMR, and determined to be novel compounds never reported in literature. Through the MTT method, high-expression human cancer cells (A549 and SGC-7901) were selected for a preliminary in vitro anti-tumor activity study on these compounds. Among them, the IC₅₀ of compound I₁ were 11.39 and 9.08 μmol/L respectively, and those of compound I₂ were 12.64 and 9.15 μmol/L respectively, which were close to those of sorafenib, a common drug for clinical use. The experimental results show that the synthesized asiatic acid derivatives have certain anti-proliferative effects on the two types of human cancer cells, A549 and SGC-7901, significantly higher than those of asiatic acid. Compounds I₁ and I₂ show quite strong anti-proliferative effects on human cancer cells A549 and SGC-7901.