Title of article
6H-Benzo[c]chromen-6-one derivatives as selective ERβ agonists
Author/Authors
Wanying Sun، نويسنده , , Lovji D. Cama، نويسنده , , Elizabeth T. Birzin، نويسنده , , Sudha Warrier، نويسنده , , Louis Locco، نويسنده , , Ralph Mosley، نويسنده , , Milton L. Hammond، نويسنده , , Susan P. Rohrer، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
1468
To page
1472
Abstract
A series of 6H-benzo[c]chromen-6-one and 6H-benzo[c]chromene derivatives were prepared, and the affinity and selectivity for ERα and ERβ was measured. Many of the analogs were found to be potent and selective ERβ 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 ERβ < 10 nM potency and >100-fold selectivity over ERα.
Keywords
ER? agonist , selective estrogen receptor modulator
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796599
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