Article
Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
Bioorganic & medicinal chemistry - 1 Jan 2012
Yamamoto Satoshi, Matsunaga Nobuyuki, Hitaka Takenori, Yamada Masami, Hara Takahito, Miyazaki Junichi, Santou Takashi, Kusaka Masami, Yamaoka Masuo, Kanzaki Naoyuki, Furuya Shuichi, Tasaka Akihiro, Hamamura Kazumasa, Ito Mitsuhiro
Abstract excerpt
A series of 4-phenylpyrrole derivatives D were designed, synthesized, and evaluated for their potential as novel orally available androgen receptor antagonists therapeutically effective against castration-resistant prostate cancers. 4-Phenylpyrrole compound 1 exhibited androgen receptor (AR) antagonistic activity against T877A and W741C mutant-type ARs as well as wild-type AR. An arylmethyl group incorporated...
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