Substituted 4-hydroxyphenyl sulfonamides as pathway-selective estrogen receptor ligands

Joseph P Sabatucci; Mark A Ashwell; Eugene Trybulski; Mary-Margaret O'Donnell; William J Moore; Douglas C Harnish; Christopher C Chadwick

doi:10.1016/j.bmcl.2005.11.015

Substituted 4-hydroxyphenyl sulfonamides as pathway-selective estrogen receptor ligands

Bioorg Med Chem Lett. 2006 Feb 15;16(4):854-8. doi: 10.1016/j.bmcl.2005.11.015. Epub 2005 Nov 21.

Authors

Joseph P Sabatucci¹, Mark A Ashwell, Eugene Trybulski, Mary-Margaret O'Donnell, William J Moore, Douglas C Harnish, Christopher C Chadwick

Affiliation

¹ Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville PA 19426, USA. [email protected]

PMID: 16300947
DOI: 10.1016/j.bmcl.2005.11.015

Abstract

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.

MeSH terms

Animals
Cell Line
Ligands
Mice
Mice, Inbred C57BL
Molecular Structure
NF-kappa B / antagonists & inhibitors*
NF-kappa B / metabolism
Receptors, Estrogen / drug effects*
Structure-Activity Relationship
Sulfonamides / chemical synthesis
Sulfonamides / chemistry
Sulfonamides / pharmacology*

Substances

Ligands
NF-kappa B
Receptors, Estrogen
Sulfonamides