具有抗肿瘤活性的青蒿酸衍生物  

Derivatives of Artemisic Acid with Antitumor Activity

作　　者：邓定安[1] 蔡俊超[1] 

机构地区：[1]中国科学院上海药物研究所,上海200031

出　　处：《有机化学》1991年第5期540-543,共4页Chinese Journal of Organic Chemistry

摘　　要：中药青蒿为菊科植物黄花蒿(Artemisiaannua L.),我国民间用于治疗疟疾,并已从中分离到抗疟药青蒿素。Artemisic acid (1) was oxidized to a six-mumbered α-methylene lactone 2 by KMnO_4.The latter 2 was further converted to the corresponding saturated lactones 4,5 by catalytic hydrogenation and polyhydroxy lactone 6 by KMnO_4 respectively.Compounds 2,3,6 showed antitumor activity against leukemia P 388 cell in vitro.whereas artemisic acid 1and saturated lactones 4 and 5 did not show activity.The growth inhibitory rate were 100%,42% for 2 and 100%,47% for 6 at the concentration of 10μg/mL,1 μg/mL respectively.

关 键 词：青蒿酸 倍半萜烯内酯 抗癌活性 

分 类 号：R979.1[医药卫生—药品]