Estrogen receptor beta-subtype selective tetrahydrofluorenones: use of a fused pyrazole as a phenol bioisostere.

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Wilkening RR, Ratcliffe RW, Fried AK, Meng D, Sun W, Colwell L, Lambert S, Greenlee M, Nilsson S, Thorsell A, Mojena M, Tudela C, Frisch K, Chan W, Birzin ET, Rohrer SP, Hammond ML

Estrogen receptor beta-subtype selective tetrahydrofluorenones: use of a fused pyrazole as a phenol bioisostere.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3896-901. Epub 2006 May 30.

PubMed ID

16730987 [ View in PubMed

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Abstract

Synthesis of a series of fused pyrazole tetrahydrofluorenone analogs which are potent, ERbeta subtype selective ligands is described. Analogs possessing subnanomolar ERbeta binding, greater than 100-fold ERbeta-selectivity, and oral bioavailability are reported.

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)	1.2	N/A	N/A	Details