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. 2018 Nov 30;9:1419. doi: 10.3389/fphar.2018.01419

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Copyright © 2018 Liu, Wu, Wang, Xie, Cui, He, He, Li, Liu, Hu, Cen and Zhou.

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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Identify IMB-A6 analogs as antiandrogens. (A) The dual-luciferase assay of AR activity in LNCaP cells for the analogs of IMB-A6. (B) The chemical structures of IMB-B2 and IMB-B5. (C) IMB-B2 demonstrated effective antiandrogenic activity in suppressing DHT-induced transcriptions of the F876L, T877A, and W741C+T877A AR mutants. (D) IMB-B5 demonstrated effective antiandrogenic activity in suppressing DHT-induced transcriptions of the F876L, T877A, and W741C+T877A AR mutants. Experiments were in triplicate. ^∗P < 0.05, ^∗∗P < 0.01 vs. DHT group. BIC, bicalutamide; HF, hydroxyflutamide; ENZ, enzalutamide; DHT, dihydrotestosterone. All results are shown as mean ± s.d.