Abstract
Through an in vivo screening model, we developed the in vivo SAR of beta-alkylthio indolyl carbinols. Through these efforts we identified a compound with potent oral in vivo efficacy in both immature and mature rat prostate weight reduction models and in a murine xenograft prostate cancer model.
MeSH terms
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Administration, Oral
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Androgen Antagonists / chemical synthesis*
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Androgen Antagonists / pharmacology*
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Animals
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Antineoplastic Agents / administration & dosage
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Antineoplastic Agents / chemical synthesis*
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Chemistry, Pharmaceutical / methods*
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Disease Models, Animal
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Drug Design
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Drug Screening Assays, Antitumor
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Male
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Methanol / analogs & derivatives*
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Methanol / chemistry*
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Mice
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Neoplasm Transplantation
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Prostatic Neoplasms / drug therapy*
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Rats
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Structure-Activity Relationship
Substances
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Androgen Antagonists
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Antineoplastic Agents
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Indoles
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Methanol