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Non-Steroidal Subtype Selective Estrogens

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The biological effects of estrogens are thought to be mediated by two receptors referred to as ERα and ERβ. In recent years significant efforts have been devoted to the design of subtype selective ligands. These ligands are valuable tools to establish the precise biological role of each of the subtypes and to develop new generations of therapeutics. The first part of this review briefly summarizes the biology behind the estrogen receptors. The second part addresses the structure-activity relationship of the subtype selective ER ligands that were reported up to now. In the third part, the current insights in the therapeutic prospects of the subtype selective estrogens will be discussed.

Keywords: estrogen receptor (er); expression; hormone receptor superfamily; hydrophobic pocket; ligand binding e-domain (lbd); pyrimidines; raloxifene; scaffolds; selective estrogen receptor modulators (serms); tamoxifen

Document Type: Review Article


Affiliations: N.V. Organon, Medicinal Chemistry Department, P.O. Box 20, 5340 BH, Oss, The Netherlands.

Publication date: May 1, 2005

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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