Estrogen Receptor Modulators: Relationships of Ligand Structure, Receptor Affinity and Functional Activity

Authors: Wallace, Owen B.¹; Richardson, Timothy I.¹; Dodge, Jeffrey A.¹

Source: Current Topics in Medicinal Chemistry, Volume 3, Number 14, October 2003 , pp. 1663-1680(18)

Publisher: Bentham Science Publishers

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Abstract:

The estrogen receptor is a regulator of a wide range of physiological functions, including the female reproductive system, in addition to bone, cardiovascular and CNS function. ER ligands have been approved for the treatment of menopausal symptoms, breast cancer and osteoporosis, however the search continues for new modulators of ER function with improved properties. Progress in medicinal chemistry programs has resulted in the identification of structurally diverse molecules with unique biological properties. Recent advances in the design and synthesis of these non-steroidal and steroidal estrogen receptor ligands is reviewed. The relationship between the structural features of the ligand and receptor function is also discussed.

Keywords: estrogen receptor modulators; steroidal estrogen receptor ligands; menopausal symptoms; estrogen receptor

Document Type: Review article

DOI: 10.2174/1568026033451727

Affiliations: 1: Lilly Research Laboratories, Indianapolis, IN 46285, USA.

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