847231-01-0Relevant academic research and scientific papers
ERβ ligands. Part 5: Synthesis and structure-activity relationships of a series of 4′-hydroxyphenyl-aryl-carbaldehyde oxime derivatives
Mewshaw, Richard E.,Bowen, S. Marc,Harris, Heather A.,Xu, Zhang B.,Manas, Eric S.,Cohn, Stephen T.
, p. 902 - 906 (2007/10/03)
A series of 4′-hydroxyphenyl-aryl-carbaldehyde oximes (5b) was prepared and found to have high affinity (4 nM) and modest selectivity (39-fold) for estrogen receptor-β (ERβ). Substitution of one of the core rings of the scaffold based around these novel ligands further expanded our knowledge in the quest toward achieving high affinity and selectivity for ERβ. An X-ray co-crystal of structure 11 revealed that the oxime moiety was mimicking the C-ring of genistein, as previously predicted by SAR and docking studies.
(4-HYDROXYPHENYL)-1H-INDOLE-3-CARBALDEHYDE OXIME DERIVATIVE AS ESTROGENIC AGENTS
-
Page/Page column 15-16, (2008/06/13)
This invention provides estrogen receptor modulators of formula (I), having the structure where R1, R2, R3, and R4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
