中文摘要：

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-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．

英文摘要：

Homocamptothecin was prepared by a novel total synthetic method in five steps from the tricyclic 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 homocamptothecin. Their structures were characterized by ^1H NMR, MS spectra and elemental analysis. Antitumor activity tests in vitro by MTT method indicated that three compounds possessed higher inhibiting activity against A-549, LOVO and MCF-7 cell lines than topotecan.