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.
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. helen_chen@merck.com
Helen Y
HY
Chen
Kevin D
KD
Dykstra
Elizabeth T
ET
Birzin
Katalin
K
Frisch
Wanda
W
Chan
Yi T
YT
Yang
Ralph T
RT
Mosley
Frank
F
DiNinno
Susan P
SP
Rohrer
James M
JM
Schaeffer
Milton L
ML
Hammond
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