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.
Lorna H Mitchell  1 ,  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
Affiliations
  • 1. Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, UK. [email protected]
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.

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