1.
Bioorg Med Chem Lett
; 16(17): 4462-6, 2006 Sep 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16815012
RESUMEN
A series of 2-9a bridged tetrahydrofluorenone derivatives were prepared which exhibited significant binding affinity for ERbeta and were highly selective.
Asunto(s)
Receptor beta de Estrógeno/química , Receptor beta de Estrógeno/metabolismo , Fluorenos/química , Hidrógeno/química , Fluorenos/síntesis química , Humanos , Ligandos , Espectroscopía de Resonancia Magnética , Conformación Molecular
2.
Bioorg Med Chem Lett
; 16(17): 4652-6, 2006 Sep 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16777408
RESUMEN
Several tetrahydrofluorenones with a triazole fused across C7-C8 showed high levels of ERbeta-selectivity and were found to be potent ERbeta-agonists. As a class they demonstrate improved oral bioavailability in the rat over a parent class of 7-hydroxy-tetrahydrofluorenones. The most selective agonist displayed 5.7 nM affinity and 333-fold selectivity for ERbeta.