Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity

Helen Y Chen; Kevin D Dykstra; Elizabeth T Birzin; Katalin Frisch; Wanda Chan; Yi T Yang; Ralph T Mosley; Frank DiNinno; Susan P Rohrer; James M Schaeffer; Milton L Hammond

doi:10.1016/j.bmcl.2004.01.031

Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1417-21. doi: 10.1016/j.bmcl.2004.01.031.

Authors

Helen Y Chen¹, Kevin D Dykstra, Elizabeth T Birzin, Katalin Frisch, Wanda Chan, Yi T Yang, Ralph T Mosley, Frank DiNinno, Susan P Rohrer, James M Schaeffer, Milton L Hammond

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. helen_chen@merck.com

PMID: 15006374
DOI: 10.1016/j.bmcl.2004.01.031

Abstract

A class of flavanoids exhibiting a high degree of selectivity for ERalpha over ERbeta has been discovered. The most active analogue 6 was found to be 66-fold ERalpha-selective and demonstrated uterine estradiol antagonism.

MeSH terms

Animals
Female
Flavonoids / chemistry*
Flavonoids / metabolism*
Humans
Protein Binding / physiology
Rats
Rats, Sprague-Dawley
Receptors, Estrogen / metabolism*
Stereoisomerism
Uterus / metabolism

Substances

Flavonoids
Receptors, Estrogen