|
|||||
|
|
Discovery of an orally-active nonsteroidal androgen receptor pure antagonist and the structure-activity relationships of its derivatives |
|
| Authors: | Tachibana Kazutaka Imaoka Ikuhiro Shiraishi Takuya Yoshino Hitoshi Nakamura Mitsuaki Ohta Masateru Kawata Hiromitsu Taniguchi Kenji Ishikura Nobuyuki Tsunenari Toshiaki Saito Hidemi Nagamuta Masahiro Nakagawa Toshito Takanashi Kenji Onuma Etsuro Sato Haruhiko |
| Institution: | Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd, Shizuoka, Japan. tachibanakzt@chugai-pharm.co.jp |
| Abstract: | 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). |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ | |