title: Synthesis and in vitro antitumor activities of xanthone derivatives containing 1,4-disubstituted-1,2,3-triazole moiety.
abstract: To explore the more active antitumor compounds, two series of new xanthones, containing 1,4-disubstituted-1,2,3-triazole moiety were designed and synthesized. Eaton's Reagent and "click reaction" were used in the synthesis. Most of the title compounds showed good inhibitory activity against the hepatoma carcinoma cell line (Bel-7402) and human cervical carcinoma cell line (HeLa) in vitro. Compounds 10a, 10e, 10f, 11r and 11t had potent activity with IC(50) values, ranging from 2.2 ± 0.17 to 7.1 ± 0.27 μM, which was equivalent to Doxorubicin.
authors.affiliation: Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Zou
authors.forename: Qingjie
authors.initials: Q
authors.lastname: Zhao
authors.forename: Honggang
authors.initials: H
authors.lastname: Hu
authors.forename: Lina
authors.initials: L
authors.lastname: Hu
authors.forename: Shichong
authors.initials: S
authors.lastname: Yu
authors.forename: Mingjuan
authors.initials: M
authors.lastname: Xu
authors.forename: Qiuye
authors.initials: Q
authors.lastname: Wu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006367:HeLa Cells; D006801:Humans; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D044004:Xanthones / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D014230:Triazoles; D044004:Xanthones