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  • Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones.

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

Bioorganic & medicinal chemistry letters (2005-05-07)
Robert E McDevitt, Michael S Malamas, Eric S Manas, Rayomand J Unwalla, Zhang B Xu, Chris P Miller, Heather A Harris
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
β-Estradiol, analytical standard
Sigma-Aldrich
β-Estradiol, BioReagent, powder, suitable for cell culture
Sigma-Aldrich
β-Estradiol, powder, γ-irradiated, suitable for cell culture
Sigma-Aldrich
β-Estradiol, ≥98%
Sigma-Aldrich
Estradiol, meets USP testing specifications