Discovery of 1H-Indole-2-carboxamides as Novel Inhibitors of the Androgen Receptor Binding Function 3 (BF3)

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• 作者：Fuqiang Ban ; Eric Leblanc ; Huifang Li ; Ravi S. N. Munuganti ; Kate Frewin ; Paul S. Rennie ; Artem Cherkasov
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：August 14, 2014
• 年：2014
• 卷：57
• 期：15
• 页码：6867-6872
• 全文大小：319K
• ISSN：1520-4804

文摘

To overcome resistance to conventional anti-androgens of human androgen receptor (AR), the allosteric site of the AR binding function 3 (BF3) was investigated as an alternative target for small molecule therapeutics. A library of 1H-indole-2-carboxamides were discovered as BF3 inhibitors and exhibited strong antiproliferative activity against LNCaP and enzalutamide-resistant prostate cancer cell lines. Several of the lead compounds may prove of particular benefit as a novel alternative treatment for castration-resistant prostate cancers.