Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.

Tachibana K; Imaoka I; Yoshino H; Kato N; Nakamura M; Ohta M; Kawata H; Taniguchi K; Ishikura N; Nagamuta M; Onuma E; Sato H

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Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.

机译：具有雄激素受体纯拮抗剂的带有羧基末端侧链的新型甾族化合物的发现与构效关系。

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Lead optimization of CH4892280 (4), an androgen receptor (AR) pure antagonist, was investigated. Compounds 6 and 7, which have a carboxylic acid at the end of the side chain at the position 7alpha of dihydrotestosterone (DHT), showed partial agonistic activities in reporter gene assay (RGA). Conversion of the steroidal core structure to 17alpha-methyltestosterone gave compound 14, which showed weak pure antagonistic activity. Optimization of the side chain by the insertion of a phenyl ring led to compounds 22 and 28-30, which showed pure antagonistic activities at submicromolar concentrations. The structure-activity relationships were clarified.

机译：研究了CH4892280（4）（一种雄激素受体（AR）纯拮抗剂）的前导优化。在二氢睾酮（DHT）7α位的侧链末端具有羧酸的化合物6和7在报告基因测定（RGA）中显示出部分激动活性。甾体核心结构向17α-甲基睾丸酮的转化得到化合物14，其显示出弱的纯拮抗活性。通过插入苯环优化侧链产生化合物22和28-30，其在亚微摩尔浓度下显示出纯的拮抗活性。阐明了结构-活性关系。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2007年第20期|共4页
作者
Tachibana K; Imaoka I; Yoshino H; Kato N; Nakamura M; Ohta M; Kawata H; Taniguchi K; Ishikura N; Nagamuta M; Onuma E; Sato H;
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正文语种 eng
中图分类药学;生物化学;
关键词
structure; Receptors; Androgen; antagonists; Bears; DHT; 受体; 雄激素; 熊;

机译：structure;Receptors;Androgen;antagonists;Bears;DHT;受体;雄激素;熊;

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1. Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists. [J] . Tachibana K, Imaoka I, Yoshino H, Bioorganic and Medicinal Chemistry Letters . 2007,第20期

机译：具有雄激素受体纯拮抗剂的带有羧基末端侧链的新型甾族化合物的发现与构效关系。
2. Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists. [J] . Yoshino H, Sato H, Tachibana K, Bioorganic and medicinal chemistry . 2010,第9期

机译：新型雄激素受体纯拮抗剂中羧酸的生物等位取代的结构活性关系。
3. Discovery of an Orally-Active Nonsteroidal Androgen Receptor Pure Antagonist and the Structure-Activity Relationships of Its Derivatives [J] . Tachibana K, Imaoka I, Shiraishi T, Chemical and Pharmaceutical Bulletin . 2008,第11期

机译：口服活性非甾体雄激素受体纯拮抗剂的发现及其衍生物的构效关系
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Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.

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