Abstract
4-((1 R,2 R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile [PF-0998425, (-)- 6a] is a novel, nonsteroidal androgen receptor antagonist for sebum control and treatment of androgenetic alopecia. It is potent, selective, and active in vivo. The compound is rapidly metabolized systemically, thereby reducing the risk of unwanted systemic side effects due to its primary pharmacology. (-)- 6a was tested negative in the 3T3 NRU assay, validating our rationale that reduction of conjugation might reduce potential phototoxicity.
MeSH terms
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Androgen Receptor Antagonists*
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Crystallography, X-Ray
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Cyclohexanols / chemical synthesis*
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Cyclohexanols / chemistry
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Cyclohexanols / pharmacology*
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Drug Design
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Ligands
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Models, Molecular
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Molecular Structure
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Nitriles / chemical synthesis*
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Nitriles / chemistry
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Nitriles / pharmacology*
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Photosensitizing Agents / chemical synthesis*
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Photosensitizing Agents / chemistry
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Photosensitizing Agents / pharmacology*
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Receptors, Androgen / chemistry
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Receptors, Androgen / metabolism
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Skin* / drug effects
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Skin* / metabolism
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Steroids / chemistry
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Structure-Activity Relationship
Substances
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4-(2-hydroxycyclohexyl)-2-(trifluoromethyl)benzonitrile
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Androgen Receptor Antagonists
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Cyclohexanols
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Ligands
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Nitriles
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Photosensitizing Agents
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Receptors, Androgen
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Steroids