title: Synthesis and biological evaluation of phenyl substituted polyoxygenated xanthone derivatives as anti-hepatoma agents.
abstract: A series of novel derivatives of phenyl substituted tetramethoxy xanthone were synthesized and evaluated for their in vitro cytotoxicity against human hepatocellular carcinoma (HCC) and non-tumor hepatic cells. Among these derivatives, compound 6 was more potent than positive control 5-fluorouracil (5-Fu) on QGY-7703 and SMMC-7721 cells with IC50 values of 6.27 μM, 7.50 μM and 15.56 μM, 14.55 μM, respectively. Furthermore, compounds 6, 14, 16, and 29 exhibited much better selectivity toward the normal hepatic cell line QSG-7701 than 5-Fu. Additionally, compound 6 significantly induced cell apoptosis in QGY-7703 cells. Our findings suggested that these phenylxanthone derivatives may hold promise as chemotherapeutic agents for the treatment of human HCC.
authors.affiliation: Department of Phytochemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
authors.forename: Ming
authors.initials: M
authors.lastname: Dai
authors.forename: Xing
authors.initials: X
authors.lastname: Yuan
authors.forename: Jian
authors.initials: J
authors.lastname: Kang
authors.forename: Zhi-Jun
authors.initials: ZJ
authors.lastname: Zhu
authors.forename: Rong-Cai
authors.initials: RC
authors.lastname: Yue
authors.forename: Hu
authors.initials: H
authors.lastname: Yuan
authors.forename: Bing-Yang
authors.initials: BY
authors.lastname: Chen
authors.forename: Wei-Dong
authors.initials: WD
authors.lastname: Zhang
authors.forename: Run-Hui
authors.initials: RH
authors.lastname: Liu
authors.forename: Qing-Yan
authors.initials: QY
authors.lastname: Sun
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000473:pathology; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D044004:Xanthones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D044004:Xanthones
keywords: Anti-hepatoma; Cytotoxic selectivity; ICZOJAIVELMTCG-UHFFFAOYSA-N; Structure–activity relationship; Xanthone