Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones.

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McDevitt RE, Malamas MS, Manas ES, Unwalla RJ, Xu ZB, Miller CP, Harris HA

Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones.

Bioorg Med Chem Lett. 2005 Jun 15;15(12):3137-42.

PubMed ID

15876535 [ View in PubMed

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Abstract

The syntheses of a series of 2-arylindene-1-ones as potent ligands of ERbeta and ERalpha are described. Several compounds exhibited high potency and moderate selectivity for the ERbeta receptor. X-ray and modeling studies were used to understand ligand binding orientation and observed affinity.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
3-BROMO-6-HYDROXY-2-(4-HYDROXYPHENYL)-1H-INDEN-1-ONE	Estrogen receptor beta	IC 50 (nM)	20	N/A	N/A	Details
Estradiol	Estrogen receptor alpha	IC 50 (nM)	3.2	N/A	N/A	Details
Estradiol	Estrogen receptor beta	IC 50 (nM)	3.6	N/A	N/A	Details