Abstract: Isopimaric-based salicylhydrazone was synthesized by the reaction of isopimaric acid (IPA) and salicylaldehyde, and characterized by IR, 1H NMR and HRMS. The cytotoxicities of target compound were evaluated against two human cancer cells (hepatoma cell HepG-2 and prostatic carcinoma cell PC-3) and a human normal liver cell L-02 in vitro using MTT method, which were compared with that of the positive drug taxol. The results showed that cytotoxic activity of isopimaric-based salicylhydrazone was similar or higher than that of taxol (IC50, 12.14 and 6.48 μmol/L) against HepG-2 and PC-3 cell lines, with IC50 values 6.50 and 9.25 μmol/L, respectively. Moreover, isopimaric-based salicylhydrazone displayed hypotoxicity to L-02 cell, with IC50 value 68.01 μmol/L, which was much lower than that of taxol (IC50, 4.02 μmol/L). The inhibitory rates and cell morphological changes showed that isopimaric-based salicylhydrazone significantly inhibited the cell proliferation in a dose-dependent manner.