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抗癌新药石蒜内铵(AT—1840)开环类似物的合成与抗癌作用研究

STRUCTURE-ACTIVIT Y-RELAFIONSHIP STUDIES OF OPEN RING ANALOGS OF THE NEW ANTICANCER AGENT LYCOBETAINE(AT—1840)

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【摘要】 石蒜内铵(lycobetaine,AT—1840)是我国学者首先发现的新结构类型的抗肿瘤药物,对卵巢癌、中晚期胃癌有较好的疗效。石蒜内铵开环类似物Ⅱ具有明显的抗癌作用。本文工作是以化合物Ⅱ做为导向化合物,进一步设计合成了一些类似化合物。以期用以寻找结构简单、作用更强的抗肿瘤物质,为进行这类化合物的抗癌机理研究,并对其在生物组织中的代谢活性研究等提供有意义的化合物。

【Abstract】 Lycobetaine (AT-1840),developed by Chinese medicinal chemists,is a new structure type of anticancer agent without obvious toxicity and side-effects,and the therapeutic effect is good in treatment of ovarial cancer and gastric cancer.The anti-cancer effects of open-ring analogs 2 of Lycobetaine were found in our previous studies.In this study,analog 2 was used as a guide compound,and some open-ring analogs of lyco- betaine were designed and synthesized in order to study their anticancer antivity and the metabolism in organic tissue.There were no obvious anticancer effects when the compounds 6a and 6b were screened against tumor in mice bearing EAC.

  • 【文献出处】 新乡医学院学报 ,Journal of Xinxiang Medical College , 编辑部邮箱 ,1988年03期
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