| 10-羟基喜树碱衍生物的合成及体外抑制肿瘤活性 |
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| 引用本文： | 李庆勇,祖元刚,付玉杰,张莹,刘群. 10-羟基喜树碱衍生物的合成及体外抑制肿瘤活性[J]. 药学学报, 2004, 39(7): 521-524 |
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| 作者姓名： | 李庆勇 祖元刚 付玉杰 张莹 刘群 |
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| 作者单位： | 1. 东北林业大学,森林植物生态学教育部重点实验室,黑龙江,哈尔滨,150040
2. 东北师范大学,化学学院,吉林,长春,130024 |
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| 基金项目： | 国家自然科学基金资助项目 ( 3 0 0 70 610 ) |
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| 摘 要： | 目的寻找高效低毒的喜树碱类抗肿瘤新药。方法合成7个喜树碱衍生物（3~9），经1HNMR，IR，MS分析确证了所合成化合物的结构，经MTT法筛选了对宫颈癌Hela、肝癌BEL-7402、胃癌7901和大肠癌CCL-187瘤株的体外抑制肿瘤活性。结果7个化合物分别对前三种瘤株有效，其中化合物4对前三种瘤株均有较好的体外抑制肿瘤细胞活性，尤其对宫颈癌Hela细胞的抑制活性大于10-羟基喜树碱。结论该类化合物的抗癌活性值得进一步研究。
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| 关 键 词： | 10-羟基喜树碱 衍生物 抗癌活性 |
| 收稿时间： | 2003-11-03 |
Synthesis and antitumor activities of 10-hydroxy camptothecin derivatives |
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| LI Qing-yong,ZU Yuan-gang,ZHANG Ying,FU Yu-jie,LIU Qun. Synthesis and antitumor activities of 10-hydroxy camptothecin derivatives[J]. Acta pharmaceutica Sinica, 2004, 39(7): 521-524 |
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| Authors: | LI Qing-yong ZU Yuan-gang ZHANG Ying FU Yu-jie LIU Qun |
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| Affiliation: | Key Laboratory of Forest Plant Ecology, Northeast Forestry University, Ministry of Education, Harbin 150040, China. |
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| Abstract: | Aim To find new anticancer drug based on the structure of 10-hydroxy camptothecin. Methods Seven camptothecin derivatives (3-9) were synthesized and the antitumor activities of these derivatives were evaluated. Results Structures of seven new compounds were determined by 1HNMR, IR, MS. Seven compounds showed inhibitory effects on Hela, BEL-7402, 7901 cell lines in vitro. Especially, compound 4 showed high bioactivities to all of the tumor cells in vitro, its anticancer activity against human cervical carcinoma Hela was much higher than that of 10-hydroxy camptothecin. Conclusion Some compounds are worth further studying. |
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| Keywords: | hydroxy camptothecin derivatives antitumor activity |
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