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

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  • Kinoyama Isao
    Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
  • Taniguchi Nobuaki
    Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
  • Kawaminami Eiji
    Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
  • Nozawa Eisuke
    Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
  • Koutoku Hiroshi
    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.
  • Okada Minoru
    Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

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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.

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