Alisiaquinones and Alisiaquinol, Dual Inhibitors of Plasmodium falciparum Enzyme Targets from a New Caledonian Deep Water Sponge

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• 作者：Denis Desoubzdanne ; Laurence Marcourt ; Roselyne Raux ; Sé ; verine Chevalley ; Dominique Dorin ; Christian Doerig ; Alexis Valentin ; Fré ; dé ; ric Ausseil ; Cé ; cile Debitus
• 刊名：Journal of Natural Products
• 出版年：2008
• 出版时间：July 2008
• 年：2008
• 卷：71
• 期：7
• 页码：1189-1192
• 全文大小：113K
• 年卷期：v.71,no.7(July 2008)
• ISSN：1520-6025

文摘

Four new meroterpenes, alisiaquinones A−C (1−3) and alisiaquinol (4), were isolated from a New Caledonian deep water sponge. Their structures and relative stereochemistry were elucidated by spectroscopic data analysis. They are related to xestoquinone, but showed unusual substitution on a tetrahydrofuran junction. They displayed micromolar range activity on two enzymatic targets of importance for the control of malaria, the plasmodial kinase Pfnek-1 and a protein farnesyl transferase, as well as on different chloroquine-sensitive and -resistant strains of Plasmodium falciparum. Alisiaquinone C displayed a submicromolar activity on P. falciparum and a competitive selectivity index on the different plasmodial strains.