针对恶性疟原虫和HL-60癌细胞的超强C-10碳青霉烯青蒿素二聚体的合成及生物学评价
Synthesis and biological evaluation of extraordinarily potent C-10 carba artemisinin dimers against P. falciparum malaria parasites and HL-60 cancer cells.
作者信息
Chadwick James, Mercer Amy E, Park B Kevin, Cosstick Richard, O'Neill Paul M
机构信息
Department of Chemistry, University of Liverpool, Liverpool, L69 7ZD, UK.
出版信息
Bioorg Med Chem. 2009 Feb 1;17(3):1325-38. doi: 10.1016/j.bmc.2008.12.017. Epub 2008 Dec 24.
PMID:19136263
Abstract
A series of artemisinin dimers incorporating a metabolically stable C-10 carba-linkage have been prepared, several of which show remarkable in vitro antimalarial activity (as low as 30 pM) versus Plasmodium falciparum and in vitro anticancer activity in the micromolar to nanomolar range versus HL-60 cell lines.
摘要
一系列含有代谢稳定的C-10碳连接键的青蒿素二聚体已被制备出来，其中几种对恶性疟原虫显示出显著的体外抗疟活性（低至30 pM），对HL-60细胞系显示出微摩尔至纳摩尔范围内的体外抗癌活性。
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