787615-76-3Relevant academic research and scientific papers
Benzopyrans as selective estrogen receptor β agonists (SERBAs). Part 4: Functionalization of the benzopyran A-ring
Norman, Bryan H.,Richardson, Timothy I.,Dodge, Jeffrey A.,Pfeifer, Lance A.,Durst, Gregory L.,Wang, Yong,Durbin, Jim D.,Krishnan, Venkatesh,Dinn, Sean R.,Liu, Shengquan,Reilly, John E.,Ryter, Kendal T.
, p. 5082 - 5085 (2008/03/14)
Benzopyrans are selective estrogen receptor (ER) β agonists (SERBAs), which bind the ER receptor subtypes α and β in opposite orientations. We have used structure based drug design to show that this unique phenomena can be exploited via substitution at the 8-position of the benzopyran A-ring to disrupt binding to ERα, thus improving ERβ subtype selectivity. X-ray cocrystal structures with ERα and ERβ are supportive of this approach to improve selectivity in this structural class.
SUBSTITUTED BENZOPYRANS AS SELECTIVE ESTROGEN RECEPTOR-BETA AGONISTS
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Page 24, (2010/02/09)
The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor ? agonists. Such agonists are useful for the treating Estrogen Receptor ? mediated diseases such as prostate cancer or BPH.
