Synthesis and biological evaluation of xanthone derivatives as anti-cancer agents targeting topoisomerase II and DNA

Topoisomerase is one of the most important targets anti-cancer drugs. In order to develop effective and low-toxic topoisomerase inhibitors, a series xanthone derivatives have been designed synthesized using principles skeleton transition. vitro cytotoxicity assays human breast cancer (MCF-7), gastric (MGC-803), cervical cancer(Hela) cell lines, compounds showed antitumor growth activity, also low toxicity normal cells L929. enzyme activity inhibition experiment, 7d 8d best inhibitory activity. The DNA binding studies disclosed that potent can intercalate into DNA, induce apoptosis in MGC-803 arrest G2/M phase. Molecular docking could bind with II through hydrogen bonds ?-stacking interactions. Graphical abstract