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

  • Eur J Med Chem. 2012 Oct:56:320-31. doi: 10.1016/j.ejmech.2012.07.051.
Wenfeng Wang  1 ,  Zedong Bai ,  Fengsen Zhang ,  Conghui Wang ,  Yaofeng Yuan ,  Jingwei Shao
Affiliations
  • 1. Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, PR China.
PMID: 22921966 DOI: 10.1016/j.ejmech.2012.07.051
Abstract

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.