Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists

descriptionPublicationkeyboard_double_arrow_right Article 01 Sep 2006 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 16, pages 4,652-4,656 (issn: 0960-894X,

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Authors: Dann L, Parker; Dongfang, Meng; Ronald W, Ratcliffe; Robert R, Wilkening; Donald M, Sperbeck; Mark L, Greenlee; Lawrence F, Colwell; +7 Authors

doi: 10.1016/j.bmcl.2006.05.103

pmid: 16777408

Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists

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Abstract

Several tetrahydrofluorenones with a triazole fused across C7-C8 showed high levels of ERbeta-selectivity and were found to be potent ERbeta-agonists. As a class they demonstrate improved oral bioavailability in the rat over a parent class of 7-hydroxy-tetrahydrofluorenones. The most selective agonist displayed 5.7 nM affinity and 333-fold selectivity for ERbeta.

Related Organizations

Merck & Co.
United States
Novum

Keywords

Fluorenes, Structure-Activity Relationship, Molecular Structure, Animals, Estrogen Receptor beta, Humans, Ligands, Azo Compounds, Rats

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