6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists.

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Sun W, Cama LD, Birzin ET, Warrier S, Locco L, Mosley R, Hammond ML, Rohrer SP

6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1468-72. Epub 2006 Jan 18.

PubMed ID

16412638 [ View in PubMed

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Abstract

A series of 6H-benzo[c]chromen-6-one and 6H-benzo[c]chromene derivatives were prepared, and the affinity and selectivity for ERalpha and ERbeta was measured. Many of the analogs were found to be potent and selective ERbeta agonists. Bis hydroxyl at positions 3 and 8 is essential for activity in a HTRF coactivator recruitment assay. Additional modifications at both phenyl rings led to compounds with ERbeta<10nM potency and >100-fold selectivity over ERalpha.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Estradiol	Estrogen receptor alpha	IC 50 (nM)	1.35	N/A	N/A	Details
Estradiol	Estrogen receptor beta	IC 50 (nM)	1.2	N/A	N/A	Details