title: [Synthesis and structure-activity relationship of cycloberberine as anti-cancer agent].
abstract: A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The primary mechanism showed that cell cycle was blocked at G2/M phase of HepG2 cells treated with 6g using flow cytometry assay. It significantly inhibited the activity of DNA Top I at the concentration of 0.1 mg mL-1. Our results provided a basis for the development of this kind of compounds as novel anti-cancer agents.
authors.forename: Chong-Wen
authors.initials: CW
authors.lastname: Bi
authors.forename: Cai-Xia
authors.initials: CX
authors.lastname: Zhang
authors.forename: Yang-Biao
authors.initials: YB
authors.lastname: Li
authors.forename: Wu-Li
authors.initials: WL
authors.lastname: Zhao
authors.forename: Rong-Guang
authors.initials: RG
authors.lastname: Shao
authors.forename: Lin
authors.initials: L
authors.lastname: Mei
authors.forename: Dan-Qing
authors.initials: DQ
authors.lastname: Song
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001599:Berberine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D004317:Doxorubicin / Q000494:pharmacology; D019008:Drug Resistance, Neoplasm; D056945:Hep G2 Cells; D006801:Humans; D061986:MCF-7 Cells; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001599:Berberine; D004317:Doxorubicin; D004264:DNA Topoisomerases, Type I