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

Hitoshi Yoshino,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

Bioorganic & Medicinal Chemistry（2010）

引用 15|浏览11

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摘要

We designed and synthesized novel AR pure antagonists for the treatment of hormone refractory prostate cancer. CH4933468 with a sulfonamide side chain showed higher activities than lead compound 5.

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关键词

Androgen receptor,Pure antagonist,Prostate cancer,Bioisostere,Sulfonamide

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