Liu Yungen, Wong Vincent Kam-Wai, Ko Ben Chi-Bun, Wong Man-Kin, Che Chi-Ming
Department of Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong, China.
Org Lett. 2005 Apr 14;7(8):1561-4. doi: 10.1021/ol050230o.
[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.
[反应：见正文] 细胞毒性青蒿素衍生物已通过“青蒿素+连接基+亲脂性烷基碳链”的模块化方法合成。揭示了碳链长度与对人肝癌细胞（HepG2）的细胞毒性之间的强相关性。值得注意的是，与青蒿素（IC50 = 97 μM）相比，通过酰胺连接基将C14H29碳链连接到青蒿素上可实现高达200倍的更强细胞毒性（IC50 = 0.46 μM）。
