Tetranortriterpenoids are the major secondary metabolites in traditional Chinese medicine from family Meliaceae and Rutaceae, which structurally featured by diverse carbon skeletons and highly oxidized degree. Two new tetranortriterpenoids, walsurobustones F (1) and G (2), were isolated from the leaves of Walsura robusta. Their structures were elucidated by 1D NMR, 2D NMR, and MS spectra. Structurally, 1 and 2 are two geometric isomers that differ at position C-22. Both 1 and 2 showed obvious antitumor activity against the cancer cell lines HL-60, SMMC-7721, A-549, MCF-7, and SW480. These findings suggest that walsurobustones F (1) and G (2) have the potential to be used as anti-cancer agents.