| 1,2,3-三氮唑类苦参碱衍生物的合成及其体外抗肿瘤活性研究 |
| |
| 引用本文： | 张晓雯,李凌宇,尚海,邹忠梅. 1,2,3-三氮唑类苦参碱衍生物的合成及其体外抗肿瘤活性研究[J]. 现代药物与临床, 2020, 35(1): 1-6 |
| |
| 作者姓名： | 张晓雯 李凌宇 尚海 邹忠梅 |
| |
| 作者单位： | 哈尔滨商业大学 药学院(药物工程技术研究中心), 黑龙江 哈尔滨 150076;中国医学科学院 北京协和医学院 药用植物研究所, 北京 100193,中国医学科学院 北京协和医学院 药用植物研究所, 北京 100193,中国医学科学院 北京协和医学院 药用植物研究所, 北京 100193;中国医学科学院 北京协和医学院 药物研究所 天然药物活性物质与功能国家重点实验室, 北京 100050,中国医学科学院 北京协和医学院 药用植物研究所, 北京 100193 |
| |
| 基金项目： | 国家自然科学基金资助项目（81502929）；中国医学科学院医学与健康科技创新工程经费资助项目（2016-I2M-3-015） |
| |
| 摘 要： | 目的设计并合成了1,2,3-三氮唑类苦参碱衍生物,并对其进行体外抗肿瘤活性研究。方法以苦参碱为起始原料,通过水解反应、N-烷基化反应、click反应等反应得到目标化合物。采用噻唑蓝(MTT)法考察所合成目标化合物对HeLa、MCF-7和HepG23种肿瘤细胞的体外抗增殖活性。结果合成了9个1,2,3-三氮唑类苦参碱衍生物,其结构经~1H-NMR,~(13)C-NMR及HR-MS确定,抗肿瘤活性测试结果表明该类化合物具有一定的抗肿瘤活性,其中化合物5h对MCF-7肿瘤细胞表现出良好的活性,且活性优于母体化合物苦参碱。结论部分目标化合物具有较好的抗肿瘤活性,为该类抗肿瘤化合物的进一步优化提供思路。
|
| 关 键 词： | 苦参碱 1,2,3-三氮唑 结构修饰 抗肿瘤活性 |
| 收稿时间： | 2019-10-16 |
Synthesis of 1,2,3-triazole-substituted matrine derivatives and their antitumor activities in vitro |
| |
| ZHANG Xiao-wen,LI Ling-yu,SHANG Hai and ZOU Zhong-mei. Synthesis of 1,2,3-triazole-substituted matrine derivatives and their antitumor activities in vitro[J]. Drugs & Clinic, 2020, 35(1): 1-6 |
| |
| Authors: | ZHANG Xiao-wen LI Ling-yu SHANG Hai ZOU Zhong-mei |
| |
| Affiliation: | College of Pharmacy(Pharmaceutical Engineering Technology Research Center), Harbin University of Commerce, Harbin 150076, China;Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China,Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China,Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China;State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China and Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100193, China |
| |
| Abstract: | Objective To devise and synthesize 1,2,3-triazole-substituted matrine derivatives and study the antitumor activities of the derivatives. Methods Taking matrine as the starting material, the target compounds were synthesized by hydrolysis reaction, N-alkylation reaction, and click reaction. Their antitumor activities of the synthesized target compounds were evaluated for HeLa, MCF-7, and HepG2 cells by MTT assay. Results Nine 1,2,3-triazole-substituted matrine derivatives were synthesized. Their structures were characterized by 1H-NMR,13C-NMR, and HR-MS. MTT assay showed that some matrine derivatives exhibited antitumor activities. Compound 5h showed good antitumor activity against MCF-7 and was superior to the parent compound matrine. Conclusion Some derivatives have good antitumor activity and provide a basis for further optimization. |
| |
| Keywords: | matrine 1,2,3-triazole structural modification antitumor activity |
| 本文献已被 CNKI 等数据库收录！ |
| 点击此处可从《现代药物与临床》浏览原始摘要信息 |
|
点击此处可从《现代药物与临床》下载全文 |
|
