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

Autor: Mitchell LH; Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, UK. lorna.mitchell@pfizer.com, Hu LY, Nguyen M, Fakhoury S, Smith Y, Iula D, Kostlan C, Carroll M, Dettling D, Du D, Pocalyko D, Wade K, Lefker B
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Apr 15; Vol. 19 (8), pp. 2176-8. Date of Electronic Publication: 2009 Mar 03.
DOI: 10.1016/j.bmcl.2009.02.104
Abstrakt: 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.
Databáze: MEDLINE