A series of novel glyco-gambogic acid(GA) compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma(HCC) cells.All compounds showed much better aqueous solubility(0.92- 1.89 mg/mL) than GA(0.013 mg/mL),and displayed potent inhibition on HCC cells(IC_(50):0.21-12.23μmol/L) and little affects on non-tumor liver cells(IC_(50):42.56-86.43μmol/L),suggesting that glyco-GA compounds selectively inhibit HCC proliferation,and may be promising candidates for further intensive study. A series of novel glyco-gambogic acid (GA) compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma (HCC) cells. All compounds showed much better aqueous solubility (0.92-1.89 mg / mL) than GA (0.013 mg / mL), and displayed potent inhibition on HCC cells (IC 50: 0.21-12.23 μmol / L) and little affects on non-tumor liver cells (IC 50: 42.56-86.43 μmol / L) suggests that glyco-GA compounds selectively inhibit HCC proliferation, and may be promising candidates for further intensive study.