| 13-酰胺基取代苦参碱衍生物的合成及抗肿瘤活性研究 |
| 投稿时间：2016-07-27 修订日期：2016-11-25 点此下载全文 |
| 引用本文：付奔,田云桃,丁力,吴秋业,郭忠武,赵庆杰.13-酰胺基取代苦参碱衍生物的合成及抗肿瘤活性研究[J].药学实践杂志,2017,35(1):12~16 |
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| 基金项目:国家自然科学基金（21502225，81102490） |
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| 中文摘要:目的 合成13-酰胺基取代苦参碱衍生物及研究该类化合物的体外抗肿瘤活性。方法 以槐果碱为原料，通过迈克尔加成（Michael addition），叠氮还原酰化反应，制得系列13-位酰胺取代的衍生物，所有化合物结构均经1H NMR等谱确证；选取人肝癌细胞（BEL-7404）和小鼠黑色素瘤细胞（K111）对所合成的目标化合物进行体外抗肿瘤药理活性筛选。结果 设计合成了9个新化合物，大多数化合物对两株肿瘤细胞都具有较强的抑制活性。结论 化合物4b和4e对人肝癌细胞（BEL-7404）有较强的抑制活性。 |
| 中文关键词:苦参碱 衍生物 合成 抗肿瘤活性 |
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| Synthesis and antitumor activity of 13-acylmatrine derivatives |
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| Abstract:Objective To synthesize a series of 13-acylmatrine derivatives and evaluate their in vitro antitumor activity.Methods Using sophocarpine as the starting material,a series of new compounds were synthesized through Michael addition,Staudinger reduction and acylation.The structure of target compounds were confirmed by 1H NMR and MS techniques. Their antitumor activity against human hepatoma cells(BEL-7404) and mice melanoma cells (K111) were evaluated in vitro by MTT assay.Results We synthesized 9 compounds and all the compounds exhibited inhibitory activities against BEL-7404 and K111.Conclusion Compound 4b and compound 4e exhibit good in vitro antitumor activity to human hepatoma cells (BEL-7404). |
| keywords:matrine derivatives synthesis antitumor activity |
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