N-Arylpiperazine-1-carboxamide Derivatives : a Novel Series of Orally Active Nonsteroidal Androgen Receptor Antagonists

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概要

• 論文の詳細を見る

• A novel series of N-arylpiperazine-1-carboxamide derivatives was synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic properties were evaluated. Reporter assays indicated that trans-2, 5-dimethylpiperazine derivatives are potent AR antagonists, and in this series trans-N-4-[4-cyano-3-(trifluoromethyl) phenyl]-N-(2, 4-difluorophenyl)-2, 5-dimethylpiperazine-1-carboxamide (18g, YM-175735) exhibited the most potent antiandrogenic activity. Compared to bicalutamide, YM-175735 is an approximately 4-fold stronger AR antagonist and has slightly increased antiandrogenic activity, suggesting that YM-175735 may be useful in the treatment of prostate cancer.

• 公益社団法人日本薬学会の論文
• 2005-04-01

著者

• Okada M

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• TANIGUCHI Nobuaki

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• Taniguchi Nobuaki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Taniguchi Nobuaki

  Drug Discovery Research Astellas Pharma Inc.

• Okada Minoru

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• KOUTOKU Hiroshi

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• Kudoh Masafumi

  Drug Discovery Research Astellas Pharma Inc.

• Kawaminami Eiji

  Medicinal Chemistry Research Ii Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.

• Kawaminami Eiji

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.ltd.

• KINOYAMA Isao

  Institute for Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• Kinoyama Isao

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• NOZAWA Eisuke

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• FURUTANI Takashi

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• KUDOH Masafumi

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• Nozawa Eisuke

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Furutani Takashi

  Institute For Drug Discovery Research Astellas Pharma Inc.

• Furutani Takashi

  Drug Discovery Research Astellas Pharma Inc.

• Koutoku Hiroshi

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Koutoku Hiroshi

  Drug Discovery Research Astellas Pharma Inc.

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