含苹果酸酯的石蒜碱衍生物的合成及生物活性  

Synthesis and Biological Activity of Lycorine Derivatives Containing Malate Ester

作　　者：赵莹 乔玲 赵国锋[1] 陈莉[1] ZHAO Ying;QIAO Ling;ZHAO Guofeng;CHEN Li(State Key Laboratory of Elemento-Organic Chemistry,College of Chemistry,Nankai University,Tianjin 300071,China)

机构地区：[1]南开大学元素有机化学国家重点实验室,化学学院,天津300071

出　　处：《高等学校化学学报》2021年第9期2789-2797,共9页Chemical Journal of Chinese Universities

基　　金：天津市自然科学基金(批准号:18JCYBJC28400)资助.

摘　　要：以具有生理活性的石蒜碱为先导化合物,设计、合成了几种含取代苹果酸酯片段的石蒜碱衍生物.所有新化合物均通过核磁共振波谱、质谱、旋光光谱及圆二色光谱进行了结构表征.抗肿瘤活性初步研究结果表明,含取代苹果酸酯的石蒜碱类似物在保持石蒜碱抗肿瘤活性的同时,对正常细胞的毒性显著下降,此结果为新型高效、低毒石蒜碱类化合物的设计奠定了基础.Several lycorine derivatives containing substituted malic acid ester segment were designed and synthesized with physiological activite lycorine as the lead compound.All new compounds were characterized by means of high resolution mass spectrometry,nuclear magnetic resonance spectroscopy,optical rotation and circular dichroism.The results of preliminary study of the antitumor activities showed that these compounds possess a significant reduction in the toxicity to normal cells while maintaining lycorine antitumor activity.This research laid a foundation for design of new type of high activity and low toxicity lycorine derivatives.

关 键 词：石蒜碱 苹果酸酯 衍生物 抗癌活性 

分 类 号：O626.25[理学—有机化学]