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

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 4, 2006, Pages 854-858

  Sabatucci, Joseph P ^a   Ashwell, Mark A ^b   Trybulski, Eugene ^a   O'Donnell, Mary Margaret ^c   Moore, William J ^a   Harnish, Douglas C ^a   Chadwick, Christopher C ^d  

^a PFIZER INC   (United States)

^b ARQULE INC   (United States)

^c NEUROGEN CORPORATION   (United States)

^d Life Diagnostics Inc   (United States)

Author keywords

Estrogen receptor; Nuclear factor B; Sulfonamide

Indexed keywords

ESTROGEN RECEPTOR; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; SULFONAMIDE;

ARTICLE; CONTROLLED STUDY; ESTROGEN ACTIVITY; HUMAN; HUMAN CELL; INFLAMMATION; MITSUNOBU REACTION; STRUCTURE ACTIVITY RELATION;

ANIMALS; CELL LINE; LIGANDS; MICE; MICE, INBRED C57BL; MOLECULAR STRUCTURE; NF-KAPPA B; RECEPTORS, ESTROGEN; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 30344447271     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.11.015     Document Type: Article

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17. 4) and concentrated. The product phenols 4 are crystallized from ethyl acetate/hexane. All compounds had NMR and MS data consistent with the proposed structures.
18. Representative examples of compounds were also screened against ERR, FXR, PPARg, PPARd,LXRa, LXRb, and VDR with no cross-activity observed at 10 uM.