Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge.
J Nat Prod
; 71(7): 1189-92, 2008 Jul.
Article
em En
| MEDLINE
| ID: mdl-18512987
ABSTRACT
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
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Poríferos
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Terpenos
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Proteínas Serina-Treonina Quinases
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Proteínas de Ciclo Celular
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Alquil e Aril Transferases
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Antimaláricos
Limite:
Animals
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Female
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Humans
Idioma:
En
Revista:
J Nat Prod
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
França