Synthesis and Pharmacological Evaluation of Novel Arylpiperazine Derivatives as Nonsteroidal Androgen Receptor Antagonists
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概要
- 論文の詳細を見る
The search for novel antiandrogens by high-throughput screening (HTS) of the Yamanouchi chemical library led to the discovery of the lead compound (5), which possesses an arylmorpholine moiety. Through the optimization of the lead compound (5), we have found a series of novel arylpiperazine derivatives. Among them, 4-[4-cyano-(3-trifluoromethyl)phenyl]-N-(4-fluorophenyl)piperazine-1-carboxamide (22 ; YM-92088) exhibited a potent AR antagonistic activity with an IC_<50> value of 0.47μм in the reporter assay, which is more potent than bicalutamide (4) which has an IC_<50> value of 0.89μм.
- 公益社団法人日本薬学会の論文
- 2004-11-01
著者
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Okada M
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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TANIGUCHI Nobuaki
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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Taniguchi Nobuaki
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Taniguchi Nobuaki
Drug Discovery Research Astellas Pharma Inc.
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Okada Minoru
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Yoden T
Institute For Technology Development Yamanouchi Pharmaceutical Co. Ltd.
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Yoden Toru
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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KOUTOKU Hiroshi
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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Kudoh Masafumi
Drug Discovery Research Astellas Pharma Inc.
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KINOYAMA Isao
Institute for Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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Kinoyama Isao
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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FURUTANI Takashi
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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KUDOH Masafumi
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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Furutani Takashi
Institute For Drug Discovery Research Astellas Pharma Inc.
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Furutani Takashi
Drug Discovery Research Astellas Pharma Inc.
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Koutoku Hiroshi
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Koutoku Hiroshi
Drug Discovery Research Astellas Pharma Inc.
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