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

Wanying Sun; Lovji D. Cama; Elizabeth T. Birzin; Sudha Warrier; Louis Locco; Ralph Mosley; Milton L. Hammond; Susan P. Rohrer

doi:10.1016/j.bmcl.2005.12.057

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

Wanying Sun, Lovji D. Cama, Elizabeth T. Birzin, Sudha Warrier, Louis Locco, Ralph Mosley, Milton L. Hammond, Susan P. Rohrer

Research output: Contribution to journal › Article › peer-review

141 Citations (SciVal)

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.

Original language	English
Pages (from-to)	1468-1472
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2005.12.057
Publication status	Published - 15-03-2006
Externally published	Yes

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Biology
Organic Chemistry
Drug Discovery
Pharmaceutical Science

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10.1016/j.bmcl.2005.12.057

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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 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.",

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AU - Sun, Wanying

AU - Cama, Lovji D.

AU - Birzin, Elizabeth T.

AU - Warrier, Sudha

AU - Locco, Louis

AU - Mosley, Ralph

AU - Hammond, Milton L.

AU - Rohrer, Susan P.

PY - 2006/3/15

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AB - 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.

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IS - 6

ER -

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

Abstract

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