Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications

    October 2008 in “ Journal of medicinal chemistry ”
    Jie Jack Li, Donna M. Iula, Maria Nguyen … Theresa Krieger-Burke
    Studysummary This study suggests that PF-0998425 is an effective androgen receptor antagonist for sebum control and androgenetic alopecia with rapid metabolism reducing the risk of systemic side effects.
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    Research cited in this study 8

    1. (1R,2S)-4-(2-Cyano-Cyclohexyl-Oxy)-2-Trifluoromethyl-Benzonitrile, A Potent Androgen Receptor Antagonist For Stimulating Hair Growth And Reducing Sebum Production Bioorganic & Medicinal Chemistry Letters · 2007
    2. Preparation of 4-Aryl-2-Trifluoromethylbenzonitrile Derivatives as Androgen Receptor Antagonists for Topical Suppression of Sebum Production Bioorganic & Medicinal Chemistry Letters · 2007
    3. Synthesis and Biological Evaluation of Amino-Pyridines as Androgen Receptor Antagonists for Stimulating Hair Growth and Reducing Sebum Production Bioorganic & Medicinal Chemistry Letters · 2007
    4. Topical Application of Ketoconazole Stimulates Hair Growth in C3H/HeN Mice The Journal of Dermatology · 2005
    5. Acne American journal of clinical dermatology · 2002
    6. Androgen Receptor Antagonists Structure-Activity Relationships Current Medicinal Chemistry · 2000
    7. Importance of Sebaceous Glands in Cutaneous Penetration of an Antiandrogen: Target Effect of Liposomes Journal of Pharmaceutical Sciences · 1997
    8. Treatment of Androgenic Disorders in Women: Acne, Hirsutism, and Alopecia Cleveland Clinic journal of medicine · 1990