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

2005; Elsevier BV; Volume: 15; Issue: 20 Linguagem: Inglês

10.1016/j.bmcl.2005.07.008

1464-3405

A. T. Vu, Stephen T. Cohn, Eric S. Manas, Heather A. Harris, Richard E. Mewshaw,

Cytokine Signaling Pathways and Interactions

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