Author/Authors :
Hitoshi Yoshino، نويسنده , , Haruhiko Sato، نويسنده , , Kazutaka Tachibana، نويسنده , , Takuya Shiraishi، نويسنده , , Mitsuaki Nakamura، نويسنده , , Masateru Ohta، نويسنده , , Nobuyuki Ishikura، نويسنده , , Masahiro Nagamuta، نويسنده , , Etsuro Onuma، نويسنده , , Toshito Nakagawa، نويسنده , , Shinichi Arai، نويسنده , , Koo-Hyeon Ahn، نويسنده , , Kyung-Yun Jung، نويسنده , , Hiromitsu Kawata، نويسنده ,
Abstract :
A series of 5,5-dimethylthiohydantoin derivatives were synthesized and evaluated for androgen receptor pure antagonistic activities for the treatment of hormone refractory prostate cancer. CH4933468 (32d) with a sulfonamide side chain not only exhibited antagonistic activity with no agonistic activity in the reporter gene assay but also inhibited the growth of bicalutamide-resistant cell lines. This compound also inhibited tumor growth of the LNCaP xenograft in mice dose-dependently.
Keywords :
Bioisostere , Androgen receptor , Pure antagonist , Prostate cancer , Sulfonamide
