| (20S)-O-硒代乙酰喜树碱衍生物的合成及其抗肿瘤活性研究 |
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| 引用本文： | 冯新江,张殊佳,王彦广. (20S)-O-硒代乙酰喜树碱衍生物的合成及其抗肿瘤活性研究[J]. 浙江大学学报(理学版), 2004, 31(4): 420-424 |
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| 作者姓名： | 冯新江 张殊佳 王彦广 |
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| 作者单位： | 浙江大学,化学系,浙江,杭州,310027 |
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| 摘 要： | 通过缩合反应合成了8个(20S)-O-硒代乙酰喜树碱衍生物(8-15),并就它们对胃癌细胞SGC-7901进行了体外抗肿瘤活性筛选,有4个新化合物具有较高的抗肿瘤活性,其中两个比喜树碱(母体化合物)或10-羟基喜树碱的活性还高.
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| 关 键 词： | 硒代乙酰喜树碱衍生物 合成 抗肿瘤活性 |
| 文章编号： | 1008-9497(2004)04-420-04 |
| 修稿时间： | 2003-11-20 |
Synthesis and antitumor activities of novel (20S)-O-selenoacetyl camptothecin derivatives |
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| FENG Xin-jiang,ZHANG Shu-jia,WANG Yan-guang. Synthesis and antitumor activities of novel (20S)-O-selenoacetyl camptothecin derivatives[J]. Journal of Zhejiang University(Sciences Edition), 2004, 31(4): 420-424 |
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| Authors: | FENG Xin-jiang ZHANG Shu-jia WANG Yan-guang |
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| Abstract: | In order to increase the stability of lactone ring of camptothecin and decrease its toxicity and remain or increase its potency of antitummors, the structure of (20S)-camptothecin was modified. Eight camptothecin analogs were synthesized by straightforward acylation of camptothecin with the corresponding acid and their antitumor activities in vitro were evaluated on human cancer cell SGC-7901 by MTT method. All the compounds were new. Biological data showed that four derivatives of camptothecin were of activity against SGC-7901 and two of them were even more potent than camptothecin or 10-hydroxycamptothecin. |
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| Keywords: | selenoacetyl camptothecin derivatives synthesis antitumor activity |
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