Synthesis and biological evaluation of aminoalcohol gambogate as anti-tumor agents

Gambogic acid(GA)was treated with corresponding dibromoalkanes to form brominated compounds, which were coupled with various amines to generate the target compounds 3a - 3t . Their structures were characterized by IR, MS and ¹H NMR. The effects of the target compounds on the proliferation of human HCC Bel-7402, SMMC-7721, Bel-7404, QGY-7701 and HepG2 cells were evaluated in vitro by MTT assay using GA and taxol as positive controls. Most of the GA derivatives( 3c , 3g , 3h , 3p , 3t )displayed more potent activity against liver cancer cells than GA, and the activities of 3g and 3h were even more potent than that of taxol.