811794-19-1Relevant articles and documents
Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists
Yoshino, Hitoshi,Sato, Haruhiko,Tachibana, Kazutaka,Shiraishi, Takuya,Nakamura, Mitsuaki,Ohta, Masateru,Ishikura, Nobuyuki,Nagamuta, Masahiro,Onuma, Etsuro,Nakagawa, Toshito,Arai, Shinichi,Ahn, Koo-Hyeon,Jung, Kyung-Yun,Kawata, Hiromitsu
, p. 3159 - 3168 (2010)
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.
IMIDAZOLIDINE DERIVATIVE
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Page/Page column 29, (2010/11/08)
The present invention provides a compound represented by formula (I): wherein n is an integer selected from 1 to 20, and R1 and R2, which may be the same or different, each represent a hydrogen atom or a linear or branched C1/s