Estrogen receptor β selective ligands: Discovery and SAR of novel heterocyclic ligands
A series of ligands with varying heterocyclic cores and substituents that display a range of selectivity's (up to >100x) for ER-β over ER-α are reported.
Chesworth, Richard,Wessel, Matthew D.,Heyden, Lisa,Mangano, F. Michael,Zawistoski, Michael,Gegnas, Laura,Galluzzo, David,Lefker, Bruce,Cameron, Kimberly O.,Tickner, Jeanne,Lu, Bihong,Castleberry, Tessa A.,Petersen, Donna N.,Brault, Amy,Perry, Pia,Ng, Oicheng,Owen, Thomas A.,Pan, Lydia,Ke, Hua-Zhu,Brown, Thomas A.,Thompson, David D.,DaSilva-Jardine, Paul
p. 5562 - 5566
(2007/10/03)
BENZIMIDAZOLE COMPOUNDS AND THEIR USE AS ESTROGEN AGONISTS/ANTAGONISTS
This invention relates to compounds, in particular benzimidazoles, that are useful as estrogen agonists and/or antagonists and pharmaceutical uses thereof. The present invention also relates to benzimidazoles that are selective for the ER? receptor and pharmaceutical uses thereof.
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Page 37
(2010/02/05)
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