ChemInform Abstract: Prenylated Xanthones as Potential P-Glycoprotein Modulators

Autor:	Marie-Geneviève Dijoux-Franca, Etienne Tsamo, Anne-Marie Mariotte, Gwenaëlle Conseil, Denis Barron, J. B. Daskiewicz, Christine Bayet, A. Di Pietro, D. Noungoue Tchamo
Rok vydání:	2000
Předmět:	chemistry.chemical_compound Cytosol Polarity (international relations) biology chemistry Prenylation Stereochemistry Direct binding Xanthone biology.protein General Medicine Decussatin P-glycoprotein
Zdroj:	ChemInform. 31
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200039127
Popis:	Dimethylallyl (DMA) derivatives of a naturally occurring xanthone (decussatin 1) were prepared. Their activity as potential P-glycoprotein inhibitors was monitored by affinity of direct binding and compared to that of corresponding DMA-flavones. Both classes of compounds exhibited the same structure-activity relationships. Decreasing polarity enhanced the binding affinity for the P-glycoprotein C-terminal cytosolic domain since DMA derivatives were more active, but unsubstituted hydroxyl group close to the carbonyl was required for efficient activity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::a58f2d26785e8e187299b2fc41a98c34 https://doi.org/10.1002/chin.200039127 Zobrazit plný text záznamu Plný text