A-ring modified betulinic acid derivatives as potent cancer preventive agents

Hsin Yi Hung, Kyoko Nakagawa-Goto, Harukuni Tokuda, Akira Iida, Nobutaka Suzuki, Ibrahim D. Bori, Keduo Qian, Kuo Hsiung Lee

研究成果: Article同行評審

10 引文 斯高帕斯(Scopus)


Ten new 3,4-seco betulinic acid (BA) derivatives were designed and synthesized. Among them, compounds 7-15 exhibited enhanced chemopreventive ability in an in vitro short-term 12-O-tetradecanoylphorbol-13-acetate (TPA) induced Epstein-Barr virus early antigen (EBV-EA) activation assay in Raji cells. Specifically, analogs with a free C-28 carboxylic acid, including 7, 8, 11, and 13, inhibited EBV-EA activation significantly. The most potent compound 8 displayed 100% inhibition at 1 × 103 mol ratio/TPA and 73.4%, 35.9%, and 8.4% inhibition at 5 × 102, 1 × 10 2, and 1 × 10 mol ratio/TPA, respectively, comparable with curcumin at high concentration and better than curcumin at low concentration. The potent chemopreventive activity of novel seco A-ring BAs (8 and 11) was further confirmed in an in vivo mouse skin carcinogenesis assay.

頁(從 - 到)1005-1008
期刊Bioorganic and Medicinal Chemistry Letters
出版狀態Published - 2014 2月 1

All Science Journal Classification (ASJC) codes

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學


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