7-Substituted umbelliferone derivatives as androgen receptor antagonists for the potential treatment of prostate and breast cancer
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- 作者：Sahar Kandil ; Kandils1@cardiff.ac.uk" class="auth_mail" title="E-mail the corresponding author ; Andrew D. Westwell ; Christopher McGuigan
- 关键词：Androgen receptor (AR) ; Prostate cancer (PC) ; Breast cancer (BC) ; Steroids ; Triple negative breast cancer (TNBC) ; Coumarin ; Umbelliferone
- 刊名：Bioorganic & Medicinal Chemistry Letters
- 出版年：2016
- 出版时间：15 April 2016
- 年：2016
- 卷：26
- 期：8
- 页码：2000-2004
- 全文大小：1893 K
文摘
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Synthesis of novel umbelliferone derivatives.
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Anti proliferative activity in human breast (MCF-7) and human prostate (22Rv1) cancer cell lines.
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50-Fold improvement over the clinical antiandrogen bicalutamide.
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Molecular modeling studies provide theoretical explanation for our findings.