Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer
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- 作者：Marcella Bassetto1 ; Salvatore Ferla ; 1 ; Ferlas1@cardiff.ac.uk" class="auth_mail" title="E-mail the corresponding author ; Fabrizio Pertusati1 ; Sahar Kandil ; Andrew D. Westwell ; Andrea Brancale ; Christopher McGuigan
- 关键词：Bicalutamide ; Enzalutamide ; Prostate cancer ; Perfluoroalkyl ; Androgen receptor ; Antiproliferative activity
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：8 August 2016
- 年：2016
- 卷：118
- 期：Complete
- 页码：230-243
- 全文大小：2452 K
文摘
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Synthesis of novel fluorinated bicalutamide and enzalutamide analogs.
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Anti-proliferative activity in four human prostate cancer cell lines improved up to 50 folds.
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Full AR antagonist effect exhibited by the new compounds.
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Activity switch from partial agonist to full AR antagonist for enobosarm scaffold.
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AR open conformation homology model and molecular modeling studies.