The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.

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Wilkening RR, Ratcliffe RW, Tynebor EC, Wildonger KJ, Fried AK, Hammond ML, Mosley RT, Fitzgerald PM, Sharma N, McKeever BM, Nilsson S, Carlquist M, Thorsell A, Locco L, Katz R, Frisch K, Birzin ET, Wilkinson HA, Mitra S, Cai S, Hayes EC, Schaeffer JM, Rohrer SP

The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. Epub 2006 May 2.

PubMed ID

16632357 [ View in PubMed

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Abstract

Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
(9aS)-4-bromo-9a-butyl-7-hydroxy-1,2,9,9a-tetrahydro-3H-fluoren-3-one	Estrogen receptor beta	IC 50 (nM)	1.5	N/A	N/A	Details
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