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15-烷亚基穿心莲内酯衍生物及其细胞毒活性

发表时间:2011-06-15  浏览量:1266  下载量:582
全部作者: 徐海伟,刘改,朱松林,戴桂馥,刘宏民
作者单位: 郑州大学药学院;郑州大学新药研究开发中心;辅仁医药科技开发有限公司
摘 要: 为研究在穿心莲内酯15位引入修饰基团后,穿心莲内酯衍生物细胞毒活性的变化,以穿心莲内酯为原料,通过脱水、缩合等反应,合成系列的15-烷亚基穿心莲内酯衍生物,评价其对Ec9706细胞的增殖抑制活性。结果表明:部分化合物对Ec9706表现出了较好的增殖抑制活性,其中化合物5b的IC50值达到了13 mg/L,与穿心莲内酯及脱水穿心莲内酯相比有明显的提高。
关 键 词: 药物化学;穿心莲内酯;15-烷亚基穿心莲内酯衍生物;细胞毒活性
Title: 15-alkylidene andrographolide derivatives and their cytotoxic activity
Author: XU Haiwei, LIU Gaizhi, ZHU Songlin, DAI Guifu, LIU Hongmin
Organization: School of Pharmaceutical Sciences, Zhengzhou University; New Drug Research & Development Center, Zhengzhou University; Furen Pharmaceutical Science and Technology Development Co., Ltd.
Abstract: In order to investigate the cytotoxic activity of 15-modification andrographolide derivatives, a series of 15-alkylidene andrographolide derivatives were synthesized by dehydration and condensation reactions with andrographolide(1) as the starting material. Their cytotoxic activity to Ec9706 was also investigated. The results showed that some of them had the cytotoxic activity to Ec9706. Compound 5b was the best one with the IC50 of 13 mg/L, which was better than that of andrographolide(1) and 11,12-didehydroandrographolide(2).
Key words: medicinal chemistry; andrographolide; 15-alkylidene andrographolide derivatives; cytotoxic activity
发表期数: 2011年6月第11期
引用格式: 徐海伟,刘改,朱松林,等. 15-烷亚基穿心莲内酯衍生物及其细胞毒活性[J]. 中国科技论文在线精品论文,2011,4(11):983-991.
 
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