Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators.

Abstract

A library of benzofurans was prepared by solid-phase synthesis methods, and several analogues were identified as potent ligands for the estrogen receptors ER-alpha and ER-beta, with some compounds having selectivity for ER-alpha. Analogues designed to more closely mimic Raloxifene were less effective. Certain benzofurans were effective in a bone pit assay, but were characterized as agonists in a MCF-7 breast tumor cell proliferation assay.

• Authors: Roger A Smith, Jinshan Chen, Mary M Mader, Ingo Muegge, Ulrike Moehler, Suresh Katti, Diana Marrero, William G Stirtan, Daniel R Weaver, Hong Xiao, William Carley
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 12 Issue 20 Pg. 2875-8 (Oct 21 2002) ISSN: 0960-894X [Print] England
• PMID: 12270167 (Publication Type: Journal Article)

Chemical References

• Benzofurans
• Estrogen Receptor alpha
• Estrogen Receptor beta
• Receptors, Estrogen
• Selective Estrogen Receptor Modulators
• Raloxifene Hydrochloride

Topics

• Benzofurans (chemical synthesis, pharmacology)
• Breast Neoplasms (drug therapy, pathology)
• Cell Line
• Drug Design
• Estrogen Receptor alpha
• Estrogen Receptor beta
• Female
• Humans
• Models, Molecular
• Raloxifene Hydrochloride (pharmacology)
• Receptors, Estrogen (drug effects)
• Selective Estrogen Receptor Modulators (chemical synthesis, pharmacology)