Structure??????activity relationships and sub-type selectivity in an oxabicyclic estrogen receptor ????/???? agonist scaffold

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• 作者：Hamann ; Lawrence G. ; Meyer ; J. Hoyt ; Ruppar ; Daniel A. ; Marschke ; Keith B. ; Lopez ; Francisco J. ; et. al.
• 关键词：Estrogen receptor ; Osteoporosis
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：March 1, 2005
• 年：2005
• 卷：15
• 期：5
• 页码：1463-1466
• 全文大小：144 K

文摘

An oxabicyclic template for estrogen receptor ?? and ?? agonists has been identified which can be tuned to provide moderate levels of selectivity for either receptor sub-type. Structure???activity relationships within this phenol-substituted oxabicyclo[3.3.1]nonene series are described. Select compounds from the present series showed activity in vivo after oral dosing in rodent models of uterine proliferation.