Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
Bioorg Med Chem Lett
; 14(11): 2741-5, 2004 Jun 07.
Article
en En
| MEDLINE
| ID: mdl-15125925
ABSTRACT
A series of estrogen receptor ligands based on a dihydrobenzoxathiin scaffold is described and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. The most active analogue, 22, was found to be 40-fold ERalpha selective in a competitive binding assay, and 22 demonstrated very potent in vivo antagonism of estradiol driven proliferation in an immature rat uterine weight gain assay.
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Bases de datos:
MEDLINE
Asunto principal:
Oxatiinas
/
Moduladores Selectivos de los Receptores de Estrógeno
/
Receptor alfa de Estrógeno
Límite:
Animals
/
Female
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
Estados Unidos