Discovery of an Orally-Active Nonsteroidal Androgen Receptor Pure Antagonist and the Structure-Activity Relationships of Its Derivatives
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概要
- 論文の詳細を見る
The 3-(4-cyano-3-trifluoromethylphenyl)-5,5-dimethylthiohydantoin derivatives which have carboxy-terminal side chains were synthesized and their agonistic/antagonistic activities against androgen receptor (AR) measured. Among them, compound 13b showed antagonistic activity (IC_<50>=130nm) with no agonistic activity even at 10000nm. This compound exhibited significant metabolic stability and oral antiandrogenic activity (ED_<50>=7mg/kg).
- 公益社団法人日本薬学会の論文
- 2008-11-01
著者
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Yoshino Hitoshi
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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小沼 悦郎
Exploratory Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Onuma Etsuro
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Onuma Etsuro
Kamakura Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Saito Hidemi
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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TACHIBANA Kazutaka
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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IMAOKA Ikuhiro
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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SHIRAISHI Takuya
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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NAKAMURA Mitsuaki
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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OHTA Masateru
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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KAWATA Hiromitsu
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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TANIGUCHI Kenji
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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ISHIKURA Nobuyuki
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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TSUNENARI Toshiaki
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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NAGAMUTA Masahiro
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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NAKAGAWA Toshito
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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TAKANASHI Kenji
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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SATO Haruhiko
Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd.
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Ohta Masateru
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Imaoka Ikuhiro
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Nakagawa Toshito
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Nakamura Mitsuaki
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Shiraishi Takuya
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Kawata Hiromitsu
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Ishikura Nobuyuki
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Nagamuta Masahiro
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Tsunenari Toshiaki
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Sato Haruhiko
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Taniguchi Kenji
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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Tachibana Kazutaka
Fuji Gotemba Research Laboratories Chugai Pharmaceutical Co. Ltd.
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