Abstract
A novel series of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles has been synthesized. The ability of these compounds to act as antagonists of the androgen receptor was investigated and several were found to have potent activity in vitro and in vivo.
Copyright 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / therapeutic use
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Cell Line, Tumor
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Drug Design
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Humans
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Male
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Nitriles / chemical synthesis
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Nitriles / chemistry*
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Nitriles / therapeutic use
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Prostatic Neoplasms / drug therapy
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Receptors, Androgen / metabolism
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Structure-Activity Relationship
Substances
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AR protein, human
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Antineoplastic Agents
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Nitriles
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Receptors, Androgen
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benzonitrile