Synthesis and tumor cytotoxicity of novel N-substituted glucosamine-bearing oleanolic acid derivatives
Synthesis and tumor cytotoxicity of novel N-substituted glucosamine-bearing oleanolic acid derivatives
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DOI：
10.1007/s40242-014-3522-3
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发表时间：
2014-05
影响因子：
3.1
通讯作者：
Li Ren;Yang Liu;Guibao Yu;Yuan Gao;X. Liu;Bo Wang;Xiaonan Deng;M. Cheng
中科院分区：
文献类型：
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作者：
Li Ren;Yang Liu;Guibao Yu;Yuan Gao;X. Liu;Bo Wang;Xiaonan Deng;M. Cheng
采用逐步糖基化的方法，设计合成了11个新的三萜皂苷类化合物，即N-取代-β-D-氨基葡萄糖苷油酸衍生物。评价了这些化合物对六种不同肿瘤细胞系的体外细胞毒活性。大多数化合物在微摩尔浓度下有效地抑制至少一种肿瘤细胞系的生长。初步的结构-活性关系（SAR）表明，酰化的氨基葡萄糖轴承三萜皂苷的氮提供的化合物，对特定的肿瘤细胞系具有高度的细胞毒性。
Eleven novel triterpenoid saponins,N-substituted-β-D-glucosaminide derivatives of oleanolic acid, were designed and synthesizedviaa stepwise glycosylation strategy. These compounds were evaluated forin vitrocytotoxic activity against six different tumor cell lines. Most of the compounds inhibited the growth of, at least, one tumor cell line effectively at micromolar concentrations. Preliminary structure-activity relationships(SARs) indicate that acylation of the nitrogen of the glucosamine-bearing triterpenoid saponins affords the compounds that are highly cytotoxic towards specific tumor cell lines.