Estrogen receptor ligands: Design and synthesis of new 2-arylindene-1-ones

Department of Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA.
Bioorganic & Medicinal Chemistry Letters (Impact Factor: 2.42). 07/2005; 15(12):3137-42. DOI: 10.1016/j.bmcl.2005.04.013
Source: PubMed


The syntheses of a series of 2-arylindene-1-ones as potent ligands of ERbeta and ERalpha are described. Several compounds exhibited high potency and moderate selectivity for the ERbeta receptor. X-ray and modeling studies were used to understand ligand binding orientation and observed affinity.

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