801233-89-6Relevant articles and documents
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.
PHENYL GUINOLINES AND THEIR USE AS ESTROGEN RECEPTOR MODULATORS
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Page 24-25, (2008/06/13)
This invention provides estrogen receptor modulators of formula: (I), having the structure wherein, R1, R2, R3, R4, R5 and R6 are as defined in the specification, or a N-oxide thereof or a pharmaceutically acceptable salt thereof or a prodrug thereof.