6H-Benzo[c]chromen-6-one Derivatives As Selective ERbeta Agonists

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2006 Jan 18

PMID 16412638

Citations 9

Authors

Wanying Sun

Lovji D Cama

Elizabeth T Birzin

Sudha Warrier

Louis Locco

Ralph Mosley

Milton L Hammond

Susan P Rohrer

Affiliations

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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.

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