Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production

Lorna H Mitchell; Lain-Yen Hu; Maria Nguyen; Stephen Fakhoury; Yvonne Smith; Donna Iula; Catherine Kostlan; Matthew Carroll; Danielle Dettling; Daniel Du; David Pocalyko; Kimberly Wade; Bruce Lefker

doi:10.1016/j.bmcl.2009.02.104

Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2176-8. doi: 10.1016/j.bmcl.2009.02.104. Epub 2009 Mar 3.

Authors

Lorna H Mitchell¹, Lain-Yen Hu, Maria Nguyen, Stephen Fakhoury, Yvonne Smith, Donna Iula, Catherine Kostlan, Matthew Carroll, Danielle Dettling, Daniel Du, David Pocalyko, Kimberly Wade, Bruce Lefker

Affiliation

¹ Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, UK. lorna.mitchell@pfizer.com

PMID: 19286380
DOI: 10.1016/j.bmcl.2009.02.104

Abstract

A series of diphenyl ethers was prepared and evaluated for androgen receptor antagonist activity in human androgen receptor binding and cellular functional assays. Analogs with potent in vitro activities were evaluated for topical in vivo efficacy in the Golden Syrian Hamster ear model. Several compounds showed reduction in wax esters in this validated animal model.

Publication types

Comparative Study

MeSH terms

Administration, Topical
Androgen Antagonists / administration & dosage*
Androgen Antagonists / chemistry*
Androgen Receptor Antagonists*
Animals
Cell Line, Tumor
Cricetinae
Humans
Male
Mesocricetus
Phenyl Ethers / administration & dosage*
Phenyl Ethers / chemical synthesis*
Receptors, Androgen / chemistry
Reproducibility of Results
Sebum / drug effects*
Sebum / metabolism*

Substances

Androgen Antagonists
Androgen Receptor Antagonists
Phenyl Ethers
Receptors, Androgen