Bioorganic & Medicinal Chemistry Letters 2003-12-15

Exploration of the bicyclo[3.3.1]nonane system as a template for the development of new ligands for the estrogen receptor.

Rajeev S Muthyala, Kathryn E Carlson, John A Katzenellenbogen

Index: Bioorg. Med. Chem. Lett. 13(24) , 4485-8, (2003)

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Abstract

Three novel structural motifs based on a bicyclo [3.3.1]nonane template were examined as new ligands for estrogen receptor (ER). Type III compounds emerged as the most promising leads for developing high-affinity ER ligands, but they showed little selectivity for either ER subtype. Type II compounds, on the other hand, despite their lower affinity, exhibited significant ERbeta binding selectivity.