Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.
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.
Mitchell
Lorna H
LH
Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, UK. lorna.mitchell@pfizer.com
Hu
Lain-Yen
LY
Nguyen
Maria
M
Fakhoury
Stephen
S
Smith
Yvonne
Y
Iula
Donna
D
Kostlan
Catherine
C
Carroll
Matthew
M
Dettling
Danielle
D
Du
Daniel
D
Pocalyko
David
D
Wade
Kimberly
K
Lefker
Bruce
B
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*
D000726:Androgen Antagonists; D059002:Androgen Receptor Antagonists; D010647:Phenyl Ethers; D011944:Receptors, Androgen