探索双环[3.3.1]壬烷体系作为开发雌激素受体新配体的模板。
Exploration of the bicyclo[3.3.1]nonane system as a template for the development of new ligands for the estrogen receptor.
作者信息
Muthyala Rajeev S, Carlson Kathryn E, Katzenellenbogen John A
机构信息
Department of Chemistry, University of Illinois, 600 S Mathews Avenue, Urbana, IL 61801, USA.
出版信息
Bioorg Med Chem Lett. 2003 Dec 15;13(24):4485-8. doi: 10.1016/j.bmcl.2003.08.061.
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.
研究了基于双环[3.3.1]壬烷模板的三种新型结构基序作为雌激素受体（ER）的新配体。III型化合物成为开发高亲和力ER配体最有前景的先导物，但它们对任何一种ER亚型的选择性都很低。另一方面，II型化合物尽管亲和力较低，但表现出显著的ERβ结合选择性。
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