Synthesis and cytotoxicity studies of artemisinin derivatives containing lipophilic alkyl carbon chains

被引：50

作者：

Liu, YG ^{[1
]}

Wong, VKW ^{[1
]}

Ko, BCB ^{[1
]}

Wong, MK ^{[1
]}

Che, CM ^{[1
]}

机构：

[1] Univ Hong Kong, Dept Chem, Hong Kong, Hong Kong, Peoples R China

来源：

ORGANIC LETTERS | 2005年 / 7卷 / 08期

关键词：

D O I：

10.1021/ol050230o

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Cytotoxic artermisinin derivatives have been synthesized by a modular approach of '' artemisinin + linker + lipophilic alkyl carbon chain ''. A strong correlation between the length of the carbon chains and the cytotoxicities against human hepatocellular carcinoma (HepG2) was revealed. Notably, compared with artemisinin (IC50 = 97 mu M), up to 200-fold more potent cytotoxicity (IC50 = 0.46 mu M) could be achieved by attachment of a C14H29 carbon chain to artemisinin via an amide linker.

引用

页码：1561 / 1564

页数：4

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