title: Design, synthesis of symmetrical bivalent mimetics of annonaceous acetogenins and their cytotoxicities.
abstract: A new series of linear dimeric compounds mimicking naturally occurring annonaceous acetogenins have been synthesized by bivalent analogue design, and their cytotoxicities have been evaluated against the growth of cancer cells by MTT method. Most of these compounds show selective action favored to human cancer cell lines over normal cell lines, and compound 9 with bis-terminal benzoquinone functionality exhibits an IC(50)=0.40 μM against MCF7 cell lines. This work mentions that appropriate conformational constraints might be a useful optimizing tool for this unique class of anticancer compounds.
authors.affiliation: Laboratory of Regenerative Biology, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, China.
authors.forename: Qicai
authors.initials: Q
authors.lastname: Xiao
authors.forename: Yongqiang
authors.initials: Y
authors.lastname: Liu
authors.forename: Yatao
authors.initials: Y
authors.lastname: Qiu
authors.forename: Zhiyi
authors.initials: Z
authors.lastname: Yao
authors.forename: Guangbiao
authors.initials: G
authors.lastname: Zhou
authors.forename: Zhu-Jun
authors.initials: ZJ
authors.lastname: Yao
authors.forename: Sheng
authors.initials: S
authors.lastname: Jiang
mesh_terms: D054378:Acetogenins / Q000737:chemistry* / Q000633:toxicity*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D016227:Benzoquinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy
chemical_list: D054378:Acetogenins; D000970:Antineoplastic Agents; D016227:Benzoquinones; C004532:quinone