title: Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.
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.
authors.affiliation: Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, UK. lorna.mitchell@pfizer.com
authors.forename: Lorna H
authors.initials: LH
authors.lastname: Mitchell
authors.forename: Lain-Yen
authors.initials: LY
authors.lastname: Hu
authors.forename: Maria
authors.initials: M
authors.lastname: Nguyen
authors.forename: Stephen
authors.initials: S
authors.lastname: Fakhoury
authors.forename: Yvonne
authors.initials: Y
authors.lastname: Smith
authors.forename: Donna
authors.initials: D
authors.lastname: Iula
authors.forename: Catherine
authors.initials: C
authors.lastname: Kostlan
authors.forename: Matthew
authors.initials: M
authors.lastname: Carroll
authors.forename: Danielle
authors.initials: D
authors.lastname: Dettling
authors.forename: Daniel
authors.initials: D
authors.lastname: Du
authors.forename: David
authors.initials: D
authors.lastname: Pocalyko
authors.forename: Kimberly
authors.initials: K
authors.lastname: Wade
authors.forename: Bruce
authors.initials: B
authors.lastname: Lefker
mesh_terms: D000287:Administration, Topical; D000726:Androgen Antagonists / Q000008:administration & dosage* / Q000737:chemistry*; D059002:Androgen Receptor Antagonists; D000818:Animals; D045744:Cell Line, Tumor; D006224:Cricetinae; D006801:Humans; D008297:Male; D008647:Mesocricetus; D010647:Phenyl Ethers / Q000008:administration & dosage* / Q000138:chemical synthesis*; D011944:Receptors, Androgen / Q000737:chemistry; D015203:Reproducibility of Results; D012629:Sebum / Q000187:drug effects* / Q000378:metabolism*
chemical_list: D000726:Androgen Antagonists; D059002:Androgen Receptor Antagonists; D010647:Phenyl Ethers; D011944:Receptors, Androgen