Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.
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.
Chen
Helen Y
HY
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. helen_chen@merck.com
Dykstra
Kevin D
KD
Birzin
Elizabeth T
ET
Frisch
Katalin
K
Chan
Wanda
W
Yang
Yi T
YT
Mosley
Ralph T
RT
DiNinno
Frank
F
Rohrer
Susan P
SP
Schaeffer
James M
JM
Hammond
Milton L
ML
D000818:Animals; D005260:Female; D005419:Flavonoids / Q000737:chemistry* / Q000378:metabolism*; D006801:Humans; D011485:Protein Binding / Q000502:physiology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011960:Receptors, Estrogen / Q000378:metabolism*; D013237:Stereoisomerism; D014599:Uterus / Q000378:metabolism
D005419:Flavonoids; D011960:Receptors, Estrogen