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

doi:10.1016/j.bmcl.2003.08.061

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

Chemistry

Research output: Contribution to journal › Article › peer-review

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 ERβ binding selectivity.

Original language	English (US)
Pages (from-to)	4485-4488
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	13
Issue number	24
DOIs	https://doi.org/10.1016/j.bmcl.2003.08.061
State	Published - Dec 15 2003

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2003.08.061

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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 ERβ binding selectivity.",

author = "Muthyala, \{Rajeev S.\} and Carlson, \{Kathryn E.\} and Katzenellenbogen, \{John A.\}",

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AU - Carlson, Kathryn E.

AU - Katzenellenbogen, John A.

N1 - This research was supported by grants from the National Institutes of Health (PHS 5R37 DK15556).

PY - 2003/12/15

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AB - 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 ERβ binding selectivity.

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

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