Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists.

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Parker DL Jr, Meng D, Ratcliffe RW, Wilkening RR, Sperbeck DM, Greenlee ML, Colwell LF, Lambert S, Birzin ET, Frisch K, Rohrer SP, Nilsson S, Thorsell AG, Hammond ML

Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4652-6. Epub 2006 Jun 13.

PubMed ID

16777408 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Estradiol	Estrogen receptor alpha	IC 50 (nM)	1.3	N/A	N/A	Details
Estradiol	Estrogen receptor beta	IC 50 (nM)	1.1	N/A	N/A	Details