Synthesis and biological activity evaluation of emodin quaternary ammonium salt derivatives as potential anticancer agents

Twenty-six emodin derivatives (17 novel) which attach quaternary ammonium salt were synthesized and evaluated for their Anticancer activities in vitro and in vivo. Compounds 11g + 12g and 11h + 12h had more significant antiproliferative ability against three Cancer cell lines and low cytotoxicity to HELF. 11g + 12g and 11h + 12h induced AGS cell Apoptosis and arrested cell cycle at the G(0)/G(1) phase in a dose-dependent manner. Furthermore, the activities of the Caspase-3, -9 Enzymes were increased in the treated cells. In vivo studies revealed that compounds 11g + 12g and 11h + 12h showed significant anti-tumor activity compared with controlled group.