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| 20(S)-O-喜树碱肉桂酸酯衍生物的合成及其抗肿瘤活性研究 | |
| 引用本文： | 段华鑫,张殊佳,周鹏.20(S)-O-喜树碱肉桂酸酯衍生物的合成及其抗肿瘤活性研究[J].有机化学,2009,29(5):724-729. |
| 作者姓名： | 段华鑫 张殊佳 周鹏 |
| 作者单位： | 1. 大连大学环境与化学工程学院,大连,116622 2. 大连大学环境与化学工程学院,大连,116622;辽宁省生物有机化学重点实验室大连,116622 |
| 摘 要： | 为了提高喜树碱内酯环的稳定性降低其毒性, 增加其抗肿瘤效能, 以喜树碱为先导化合物, 通过酯化反应直接合成了17个20(S)-喜树碱肉桂酸酯衍生物, 并采用MTT法测定了对于人胃癌细胞SGC-7901的体外抗肿瘤活性, 活性测试结果表明有些化合物的抑制活性明显高于母体化合物喜树碱. |
| 关 键 词： | 喜树碱衍生物 肉桂酸 合成 抗肿瘤活性 |
| 收稿时间： | 2008-8-3 |
| 修稿时间： | 2008-10-29 |
Synthesis and Antitumor Activity of 20(S)-O-Linked Camptothecin Cinnamic Acid Ester Derivatives |
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| Duan,Huaxin,Zhang,Shujia,Zhou,Peng.Synthesis and Antitumor Activity of 20(S)-O-Linked Camptothecin Cinnamic Acid Ester Derivatives[J].Chinese Journal of Organic Chemistry,2009,29(5):724-729. | |
| Authors: | Duan Huaxin Zhang Shujia Zhou Peng |
| Institution: | (a College of Environmental and Chemical Engineering, Dalian University, Dalian 116622) (b Key Laboratory of Bioorganic Chemistry of Liaoning Province, Dalian 116622) |
| Abstract: | In order to increase the stability of lactone ring of camptothecin and decrease its toxicity or increase its potency of antitummors, the camptothecin structure was modified and 17 camptothecin cinnamic acid ester derivatives were synthesized by straightforward esterification of camptothecin with the corresponding acid. And their antitumor activities in vitro were evaluated against human cancer cell SGC-7901 by a MTT method. The preliminary experimental results showed that the bioactivities of some derivatives of campto-thecin were higher than that of their parent against SGC-7901. |
| Keywords: | camptothecin derivative cinnamic acid synthesis antitumor activi |
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