| 沙蟾毒精酯类衍生物的合成和抗肿瘤活性研究 |
| 投稿时间：2020-07-06 修订日期：2020-09-28 点此下载全文 |
| 引用本文：罗川,马建江,缪震元,吴岳林.沙蟾毒精酯类衍生物的合成和抗肿瘤活性研究[J].药学实践杂志,2021,39(1):35~37,57 |
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| 基金项目:安徽省科技重大专项（201903a07020031） |
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| 中文摘要:目的 基于活性天然产物沙蟾毒精骨架设计3-酯类衍生物，并测试其抗肿瘤活性。方法 通过缩合剂催化下将酸和沙蟾毒精进行酯化反应，得到3-酯类沙蟾毒精衍生物，采用Cell Titer法测试体外抗肿瘤活性。结果 3-沙蟾毒精酯类衍生物对所有的肿瘤细胞株显示出优异的体外抗肿瘤活性，其IC50值均在1 μmol/L以下。结论 化合物2a活性最好，对3种肿瘤细胞株的IC50值为4.0～91.7 nmol/L，可作为抗肿瘤候选化合物进行进一步研究。 |
| 中文关键词:沙蟾毒精 药物设计 酯类 抗肿瘤活性 |
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| Design, synthesis and antitumor activity of 3-arenobufagin esters |
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| Abstract:Objective To search for novel potent 3-ester derivatives of arenobufagin and test their antitumor activities in vitro.Methods Target compounds were synthesized by esterification of arenobufagin with acids. CellTiter method was used to assay the in vitro antitumor activities.Results 3-Ester derivatives exhibited excellent antitumor activities against all the cancer cells.Conclusion Among the 3-ester derivatives, compound 2a had the best activities with the IC50 of 4.0−91.7 nmol/L and appeared to be a valuable candidate for further study. |
| keywords:arenobufagin drug design ester derivatives antitumor activity |
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