ERβ ligands. Part 4: Synthesis and structure–activity relationships of a series of 2-phenylquinoline derivatives

…, ST Cohn, ES Manas, HA Harris, RE Mewshaw

Index: Vu, An T.; Cohn, Stephen T.; Manas, Eric S.; Harris, Heather A.; Mewshaw, Richard E. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 20 p. 4520 - 4525

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Citation Number: 55

Abstract

A new class of estrogen receptor β (ERβ) ligands based on the 2-phenylquinoline scaffold was prepared. Several analogues with C4 substitution displayed high affinity (3–5nM) and significant selectivity (up to 83-fold) for ERβ. The best compound, 13b, was profiled as a selective partial agonist for ERβ at 1μM in a cell-based transcriptional assay. Uterine weight bioassay of 13b indicated no activation of ERα in vivo.