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Synthesis and Cytotoxic Activity of Pentacyclic Triterpenoid Sulfamates

机译:五环三萜磺酸酯的合成及细胞毒活性

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Methyl triterpenoates derived from oleanolic, ursolic, betulinic, glycyrrhetinic, platanic, or maslinic acid were converted into their corresponding sulfamates and carbamoylsulfamates. The sulfamates were screened in photometric sulforhodamine assays for cytotoxic activity employing several human tumor cell lines. Many of the compounds showed EC50 values in one-digit mu M concentration. Of special interest seems methyl (3 beta) 3-(aminosulfonyloxy)-11-oxo-oleanoate (18) showing good cytotoxicity for the human adenocarcinomic alveolar basal epithelial cell line A549 while being less toxic for non-malignant NIH 3T3 mouse fibroblasts.
机译:衍生自齐墩果酸,熊果酸,桦木酸,甘草次酸,铂酸或山梨酸的三萜烯酸甲酯被转化为其相应的氨基磺酸盐和氨基甲酰基氨基磺酸盐。使用几种人类肿瘤细胞系,在光度磺基罗丹明分析中筛选了氨基磺酸盐的细胞毒性活性。许多化合物的EC50值均以一位M浓度表示。特别令人感兴趣的似乎是(3 beta)3-(氨基磺酰氧基)-11-氧-油酸甲酯(18)对人腺癌的肺泡基底细胞上皮细胞系A549显示良好的细胞毒性,而对非恶性NIH 3T3小鼠成纤维细胞的毒性较小。

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