1108181-04-9Relevant academic research and scientific papers
Discovery of an orally-active nonsteroidal androgen receptor pure antagonist and the structure-activity relationships of its derivatives
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
experimental part, p. 1555 - 1561 (2009/10/10)
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).
