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).