title: Synthesis of novel benzoxanthone analogues as non-Camptothecin topoisomerase I inhibitors.
abstract: Structure modification of the side chain of the lead compound benzoxanthone provided a series of benzoxanthone analogues and 12 of them were first reported. The results showed that most of these compounds had moderate cytotoxicity against tumour cells with the 50% inhibition concentration in the micromolar range. Furthermore, benzoxanthone derivatives 5, 6c, 7a and 7e, showed potent topoisomerase I (Topo I) inhibitory effect and the results indicated that some compounds had potential for development as non-Camptothecin (CPT) topoisomerase I inhibitors.
authors.affiliation: School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.
authors.forename: Pengfei
authors.initials: P
authors.lastname: Cheng
authors.forename: Lingjian
authors.initials: L
authors.lastname: Zhu
authors.forename: Wei
authors.initials: W
authors.lastname: Guo
authors.forename: Wenfeng
authors.initials: W
authors.lastname: Liu
authors.forename: Jianzhong
authors.initials: J
authors.lastname: Yao
authors.forename: Guoqiang
authors.initials: G
authors.lastname: Dong
authors.forename: Yongqiang
authors.initials: Y
authors.lastname: Zhang
authors.forename: Chunlin
authors.initials: C
authors.lastname: Zhuang
authors.forename: Chunquan
authors.initials: C
authors.lastname: Sheng
authors.forename: Zhenyuan
authors.initials: Z
authors.lastname: Miao
authors.forename: Wannian
authors.initials: W
authors.lastname: Zhang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D044004:Xanthones / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D059004:Topoisomerase I Inhibitors; D044004:Xanthones; D004264:DNA Topoisomerases, Type I