Abstract:
:The phenolic "A-ring" of natural and synthetic estrogen receptor (ER) ligands was effectively replaced by a planar six-member ring formed through an intramolecular hydrogen bond within a salicylaldoxime. Thus, oxime 1, a structural analogue of a triarylethylene estrogen, showed a significant binding affinity for the ER. The OH of the oxime function appears to mimic the phenolic OH present in more "classical" ER ligands because the binding reduced when the oxime OH is methylated (2) or absent (3).
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Minutolo F,Bertini S,Papi C,Carlson KE,Katzenellenbogen JA,Macchia Mdoi
10.1021/jm010948jkeywords:
subject
Has Abstractpub_date
2001-11-22 00:00:00pages
4288-91issue
24eissn
0022-2623issn
1520-4804pii
jm010948jjournal_volume
44pub_type
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