Substituted 4-hydroxyphenyl sulfonamides as pathway-selective estrogen receptor ligands.
The transcription factor nuclear factor-kappaB (NF-kappaB) is a key component in the onset of inflammation. We describe here a series of 4-hydroxyphenyl sulfonamide estrogen receptor (ER) ligands that selectively inhibit NK-kappaB transcriptional activity but are devoid of conventional estrogenic activity.
Sabatucci
Joseph P
JP
Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville PA 19426, USA. sabatuj@wyeth.com
Ashwell
Mark A
MA
Trybulski
Eugene
E
O'Donnell
Mary-Margaret
MM
Moore
William J
WJ
Harnish
Douglas C
DC
Chadwick
Christopher C
CC
D000818:Animals; D002460:Cell Line; D008024:Ligands; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011960:Receptors, Estrogen / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D008024:Ligands; D016328:NF-kappa B; D011960:Receptors, Estrogen; D013449:Sulfonamides