Synthesis and binding affinity to human α and β estrogen receptors of various 7-hydroxycoumarins substituted at 4- and 3,4- positions

Synthesis and binding affinity to human α and β estrogen receptors of various 7-hydroxycoumarins substituted at 4- and 3,4- positions

The study of the relative binding affinity (RBA) to the human α and β estrogen receptors (ERs) of various 7-hydroxycoumarins substituted at 4- and 3,4- positions is weak and lacks in selectivity for both ERα and ERβ. The 4-(4-hydroxyphenyl)-7-hydroxycoumarin shows a weak RBA to ERβ and 3,4-diphenyl-...

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Veröffentlicht in:Farmaco (Società chimica italiana : 1989) 2004-12, Vol.59 (12), p.981-986
Hauptverfasser: Kirkiacharian, Serge, Lormier, Anh Tuan, Chidiack, Henri, Bouchoux, Françoise, Cérède, Evelyne
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Binding affinity
Cercopithecus aethiops
COS Cells
Estrogen Receptor alpha - metabolism
Estrogen Receptor beta - metabolism
Humans
Protein Binding - physiology
Substituted-7-hydroxycoumarins
Umbelliferones - chemical synthesis
Umbelliferones - metabolism
α and β estrogen receptors
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Zusammenfassung:The study of the relative binding affinity (RBA) to the human α and β estrogen receptors (ERs) of various 7-hydroxycoumarins substituted at 4- and 3,4- positions is weak and lacks in selectivity for both ERα and ERβ. The 4-(4-hydroxyphenyl)-7-hydroxycoumarin shows a weak RBA to ERβ and 3,4-diphenyl-7-hydroxycoumarin presents a stronger RBA to ERα than ERβ.
ISSN:0014-827X
1879-0569
DOI:10.1016/j.farmac.2004.08.004