文献一覧: Mitsuaki Nakamura (著者)

1 0 0 0 OA Discovery of an Orally-Active Nonsteroidal Androgen Receptor Pure Antagonist and the Structure–Activity Relationships of Its Derivatives

著者: Kazutaka Tachibana Ikuhiro Imaoka Takuya Shiraishi Hitoshi Yoshino Mitsuaki Nakamura Masateru Ohta Hiromitsu Kawata Kenji Taniguchi Nobuyuki Ishikura Toshiaki Tsunenari Hidemi Saito Masahiro Nagamuta Toshito Nakagawa Kenji Takanashi Etsuro Onuma Haruhiko Sato
出版者: The Pharmaceutical Society of Japan
雑誌: Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日: vol.56, no.11, pp.1555-1561, 2008-11-01 (Released:2008-11-01)
参考文献数: 21
被引用文献数: 14 20

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 (IC50=130 nM) with no agonistic activity even at 10000 nM. This compound exhibited significant metabolic stability and oral antiandrogenic activity (ED50=7 mg/kg).

2018-06-04 07:05:25
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1 0 0 0 OA Errata: Discovery of an Orally-Active Nonsteroidal Androgen Receptor Pure Antagonist and the Structure–Activity Relationships of Its Derivatives [Chem. Pharm. Bull. 56(11): 1555-1561 (2008)]

1 0 0 0 OA Discovery of an Orally-Active Nonsteroidal Androgen Receptor Pure Antagonist and the Structure–Activity Relationships of Its Derivatives