787615-76-3Relevant articles and documents
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.
