Synthesis and cytotoxicity studies of artemisinin derivatives containing lipophilic alkyl carbon chains |
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Authors: | Liu Yungen Wong Vincent Kam-Wai Ko Ben Chi-Bun Wong Man-Kin Che Chi-Ming |
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Affiliation: | Department of Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong, China. |
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Abstract: | [reaction: see text] 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 (IC(50) = 97 microM), up to 200-fold more potent cytotoxicity (IC(50) = 0.46 microM) could be achieved by attachment of a C(14)H(29) carbon chain to artemisinin via an amide linker. |
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