Article
A novel small-molecule androgen receptor antagonist selective for the T878A-mutant AR in prostate cancer therapy.
European journal of medicinal chemistry - 5 Aug 2026
Zheng Yangyang, Chai Xin, Wang Huating, Yan Zihan, Lin Zhaoyang, Shan Luhu, Wang Xinyue, Du Ganpeng, Ren Qunce, Xu Xiaohong, Chen Wenteng, Hou Tingjun, Li Dan
Abstract excerpt
Prostate cancer (PCa) is one of the most prevalent malignancies in males. While androgen receptor (AR) antagonists play a crucial role in PCa therapy, their efficacy is often limited by resistance arising from AR mutations. Here, we identified S-94, corresponding to the S-enantiomer of compound 94, as a novel AR antagonist with marked selectivity for the T878A-mutant AR. In vitro, S-94 inhibited AR...
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