Objective To modify the double bonds and hydroxyl groups of marine natural product brefeldin A(1),derivatives 2-10 were prepared and their inhibitory activities against lung adenocarcinoma epithelial A549 cells were evaluated.Methods The cytotoxic activities of all derivatives(2-10)against lung adenocarcinoma epithelial A549 were evaluated using an MTT assay.Results Derivatives 2-7 and 8-10 were designed and synthesized by introducing sulfur atoms and acetylation into the structure of compound 1,respectively.All derivatives could inhibit the growth of A549 cells below 1 μmol/L,among which derivatives 8 and 9 exhibited significant activities,with the half maximal inhibitory concentration IC50 values of 422 and 127 nmol/L respectively,which could be used as potential anticancer lead compounds.
关键词
结构修饰/brefeldin/A衍生物/细胞毒活性/海洋天然产物
Key words
structural modification/brefeldin A derivatives/cytotoxic activity/marine natural product
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