Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators.
J Med Chem
; 47(9): 2171-5, 2004 Apr 22.
Article
en En
| MEDLINE
| ID: mdl-15084115
ABSTRACT
The discovery and synthesis of dihydrobenzoxathiins as potent, ERalpha subtype selective ligands are described. The most active analogue, 4-D, was found to be 50-fold selective in a competitive binding assay and 100-fold selective in a transactivation assay in HEK-293 cells. The alpha selectivity was postulated to lie in the interaction of the sulfur atom of the benzoxathiin ring with the two discriminating residues in the binding pocket of the receptor isoforms.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Oxatiinas
/
Moduladores Selectivos de los Receptores de Estrógeno
Límite:
Animals
/
Female
/
Humans
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
Estados Unidos