Synthesis and biological evaluation of glyco-GA compounds as anticancer agents

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 (IC50: 0.21–12.23 μmol/L) and little affects on non-tumor liver cells (IC50: 42.56–86.43 μmol/L), suggesting that glyco-GA compounds selectively inhibit HCC proliferation, and may be promising candidates for further intensive study.