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药学学报  2015 

齐墩果酸衍生物的合成及抗肿瘤活性研究

, PP. 469-474

Keywords: 齐墩果酸,五环三萜类化合物,抗肿瘤活性

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Abstract:

以天然产物齐墩果酸为起始原料,对其c-3位羟基、c-12位双键、c-28位羧基进行结构改造,合成了13个新的齐墩果酸衍生物.目标化合物结构经ms、1hnmr及元素分析确证.采用mtt法,选用高表达人癌细胞(sgc7901、mcf-7和a549)对目标化合物进行初步的体外抗肿瘤活性研究.结果表明,所测化合物对3种肿瘤细胞的抑制活性均明显强于齐墩果酸,其中化合物ii2和ii3对mcf-7和a549细胞表现出很强的抑制活性,明显高于已上市药物吉非替尼,值得进一步研究.

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