ERβ ligands. Part 5: Synthesis and structure–activity relationships of a series of 4′-hydroxyphenyl-aryl-carbaldehyde oxime derivatives

RE Mewshaw, SM Bowen, HA Harris, ZB Xu…

文献索引：Mewshaw, Richard E.; Bowen, S. Marc; Harris, Heather A.; Xu, Zhang B.; Manas, Eric S.; Cohn, Stephen T. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 4 p. 902 - 906

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被引用次数: 22

摘要

A series of 4′-hydroxyphenyl-aryl-carbaldehyde oximes (5b) was prepared and found to have high affinity (4nM) 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- ...