2. Academic Validation
  3. Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists

Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists

  • Bioorg Med Chem. 2010 May 1;18(9):3159-68. doi: 10.1016/j.bmc.2010.03.036.
Hitoshi Yoshino 1,  Haruhiko Sato,  Kazutaka Tachibana,  Takuya Shiraishi,  Mitsuaki Nakamura,  Masateru Ohta,  Nobuyuki Ishikura,  Masahiro Nagamuta,  Etsuro Onuma,  Toshito Nakagawa,  Shinichi Arai,  Koo-Hyeon Ahn,  Kyung-Yun Jung,  Hiromitsu Kawata
Affiliations

Affiliation

  • 1 Research Division, Chugai Pharmaceutical Co., Ltd, 1-135, Komakado, Gotemba, Shizuoka 412-8513, Japan. yoshinohts@chugai-pharm.co.jp
PMID: 20381361 DOI: 10.1016/j.bmc.2010.03.036
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.

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