Synthesis and Cytotoxicity Studies of Artemisinin Derivatives Containing Lipophilic Alkyl Carbon Chains
- 18 March 2005
- journal article
- letter
- Published by American Chemical Society (ACS) in Organic Letters
- Vol. 7 (8) , 1561-1564
Abstract
Cytotoxic artemisinin 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 μM), up to 200-fold more potent cytotoxicity (IC50 = 0.46 μM) could be achieved by attachment of a C14H29 carbon chain to artemisinin via an amide linker.Keywords
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