| 10-酯基高喜树碱的全合成及抗肿瘤活性研究 |
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| 引用本文： | 缪震元,张万年,姚建忠,盛春泉,徐辉,张珉,张晶,游亮,车晓颖.10-酯基高喜树碱的全合成及抗肿瘤活性研究[J].有机化学,2006,26(9):1221-1224. |
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| 作者姓名： | 缪震元 张万年 姚建忠 盛春泉 徐辉 张珉 张晶 游亮 车晓颖 |
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| 作者单位： | 中国人民解放军第二军医大学药学院,上海,200433 |
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| 基金项目： | 国家自然科学基金(No.30371689)资助项目. |
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| 摘 要： | 以2,8-二氧-3-乙基-6,6-亚乙二氧基-2,3,5,6,7,8-六氢-3-羟基吡喃(5,4-c)中氮茚为起始原料, 经五步反应得到高喜树碱, 羟甲基化后与一系列酸成酯合成了6个10-酯基高喜树碱, 并利用1H NMR, MS及元素分析对其结构进行了表征. 采用经典的噻唑兰(Thiazoly blue tetrazolium bromide, MTT)法测定了其体外抗肿瘤活性, 活性测试结果表明3个化合物具有比阳性对照药拓扑替康增强的活性.
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| 关 键 词： | 10-酯基高喜树碱 全合成 抗肿瘤活性 |
| 收稿时间： | 12 6 2005 12:00AM |
| 修稿时间： | 03 6 2006 12:00AM |
Synthesis and Antitumor Activity of 10-Ester Derivatives of Homocamptothecin |
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| MIAO Zhen-Yuan,ZHANG Wan-Nian,YAO Jian-Zhong,SHENG Chun-Quan,XU Hui,ZHANG Min,ZHANG Jing,YOU Liang,CHE Xiao-Ying.Synthesis and Antitumor Activity of 10-Ester Derivatives of Homocamptothecin[J].Chinese Journal of Organic Chemistry,2006,26(9):1221-1224. |
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| Authors: | MIAO Zhen-Yuan ZHANG Wan-Nian YAO Jian-Zhong SHENG Chun-Quan XU Hui ZHANG Min ZHANG Jing YOU Liang CHE Xiao-Ying |
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| Institution: | (School of Pharmacy, Second Military Medical University of the People’s Liberation Army of China, Shanghai 200433) |
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| Abstract: | Homocamptothecin was prepared by a novel total synthetic method in five steps from the tri- cyclic starting material 2,8-dioxo-3-ethyl-6,6-ethylenedioxy-2,3,5,6,7,8-hexahydro-3-hydroxypyrano(5,4- c)indolizine. Hydrogen peroxide oxidized homocamptothecin with methanol to form 10-hydroxymethyl- homocamptothecin, which then reacted with a series of acids to afford six 10-ester derivatives of homo- camptothecin. Their structures were characterized by 1H NMR, MS spectra and elemental analysis. Antitu- mor activity tests in vitro by MTT method indicated that three compounds possessed higher inhibiting activ- ity against A-549, LOVO and MCF-7 cell lines than topotecan. |
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| Keywords: | 10-ester-homocamptothecin total synthesis antitumor activity |
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