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ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives.

Abstract：

: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-beta (ERbeta). 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 ERbeta. 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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Mewshaw RE,Bowen SM,Harris HA,Xu ZB,Manas ES,Cohn ST

doi

10.1016/j.bmcl.2006.11.066

subject

Has Abstract

pub_date

2007-02-15 00:00:00

pages

902-6

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)01354-0

journal_volume

17

pub_type

杂志文章

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