801233-48-7Relevant academic research and scientific papers
ERβ ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives
Vu, An T.,Cohn, Stephen T.,Manas, Eric S.,Harris, Heather A.,Mewshaw, Richard E.
, p. 4520 - 4525 (2007/10/03)
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 (3-5 nM) and significant selectivity (up to 83-fold) for ERβ. The best compound, 13b, was profiled as a selective partial agonist for ERβ at 1 μM in a cell-based transcriptional assay. Uterine weight bioassay of 13b indicated no activation of ERα in vivo.
