期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 57, 期 15, 页码 6867-6872出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm500684r
关键词
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资金
- Prostate Cancer Canada
- Canada Safeway Grant [SP2013-02]
- Department of Defense (Prostate Cancer Research Program) Award [W81XWH-12-1-0401]
- Canadian Institutes of Health Research
- Canadian Cancer Society Research Institute Grant [F12-03271]
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.
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