(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production.
Synthesis, pharmacology, and pharmacokinetic profiles of (1R, 2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile are reported. This compound demonstrated remarkable potency for stimulating hair growth in a male C3H mouse model as well as reducing sebum production in the male Syrian hamster ear model.
Hu
Lain-Yen
LY
Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. lain-yen.hu@pfizer.com
Du
Daniel
D
Hoffman
Jennifer
J
Smith
Yvonne
Y
Fedij
Victor
V
Kostlan
Catherine
C
Johnson
Theodore R
TR
Huang
Yun
Y
Kesten
Steve
S
Harter
William
W
Yue
Wen Song
WS
Li
Jie Jack
JJ
Barvian
Nicole
N
Mitchell
Lorna
L
Lei
Huangshu John
HJ
Lefker
Bruce
B
Carroll
Mathew
M
Dettling
Danielle
D
Krieger-Burke
Teresa
T
Samas
Brian
B
Yalamanchili
Radhika
R
Lapham
Kimberly
K
Pocalyko
David
D
Sliskovic
Drago
D
Ciotti
Susan
S
Stoller
Brenda
B
Hena
Mostofa A
MA
Ding
Qizhu
Q
Maiti
Samarendra N
SN
Stier
Michael
M
Welgus
Howard
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D000726:Androgen Antagonists / Q000494:pharmacology*; D000818:Animals; D006224:Cricetinae; D006197:Hair / Q000254:growth & development*; D006845:Hydrocarbons, Fluorinated / Q000493:pharmacokinetics / Q000494:pharmacology*; D008297:Male; D008647:Mesocricetus; D051379:Mice; D008958:Models, Molecular; D009570:Nitriles / Q000493:pharmacokinetics / Q000494:pharmacology*; D012629:Sebum