title: Synthesis and biological activity evaluation of emodin quaternary ammonium salt derivatives as potential anticancer agents.
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.
authors.affiliation: Institute of Organic Chemistry, College of Chemistry and Chemical Engineering, Fuzhou University, Fujian 350108, PR China.
authors.forename: Wenfeng
authors.initials: W
authors.lastname: Wang
authors.forename: Zedong
authors.initials: Z
authors.lastname: Bai
authors.forename: Fengsen
authors.initials: F
authors.lastname: Zhang
authors.forename: Conghui
authors.initials: C
authors.lastname: Wang
authors.forename: Yaofeng
authors.initials: Y
authors.lastname: Yuan
authors.forename: Jingwei
authors.initials: J
authors.lastname: Shao
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004642:Emodin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D008114:Liver Neoplasms, Experimental / Q000188:drug therapy*; D051379:Mice; D008815:Mice, Inbred Strains; D015394:Molecular Structure; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012492:Salts / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D000644:Quaternary Ammonium Compounds; D012492:Salts; D004642:Emodin