Structural modification of isoalantolactone and biological activity against the hepatoma cell lines

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  • Rui-Xia Guo
    School of Pharmaceutical Sciences, Hebei Key Laboratory of Forensic Medicine, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, P.R. China
  • Li-Geng Li
    School of Pharmaceutical Sciences, Hebei Key Laboratory of Forensic Medicine, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, P.R. China
  • Man-Li Zhang
    School of Pharmaceutical Sciences, Hebei Key Laboratory of Forensic Medicine, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, P.R. China
  • Françoise Sauriol
    Department of Chemistry, Queen’s University, Kingston, Ontario, K7L 3N6, Canada
  • Qing-Wen Shi
    School of Pharmaceutical Sciences, Hebei Key Laboratory of Forensic Medicine, Hebei Medical University, Shijiazhuang, Hebei Province, 050017, P.R. China
  • Yu-Cheng Gu
    Syngenta Jealott’s Hill International Research Centre, Berkshire, RG42 6EY, UK
  • Hiromasa Kiyota
    Graduate School of Environmental and Life Science, Okayama University, 1-1-1 Tsushima-Naka, Kita-ku, Okayama 700-8530, Japan

抄録

<jats:title>Abstract</jats:title> <jats:p>Structural modifications were performed on isoalantolactone in an effort to find compounds with potential anticancer activity. Seven previously unknown adducts of active methylene compounds with isoalantolactone were synthesized by the Michael reaction. Moreover, four derivatives of aryl-substituted isoalantolactone were prepared by the Heck reaction. All synthetic products were evaluated for toxic activities against three different hepatoma cell lines, Bel-7402, SMMC-7721, and Hep G2. Products prepared through the Heck reaction and <jats:bold>3a,b</jats:bold> show potential antiproliferative activity against the Hep G2 cell.</jats:p>

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