Fig. 1: Synthesis of niclosamide analogs and identification of potent inhibitors of AR/AR variants.
From: ARVib suppresses growth of advanced prostate cancer via inhibition of androgen receptor signaling
A The chemical structure of niclosamide and newly synthesized ARVibs. The red box indicates the structures of #7 and #31, the green box indicates chemical structures of #1 and #34. B CWR22Rv1 cells were treated with 1 µM ARVib for 16 h and whole-cell lysates were collected and subjected to western blot. C C4-2B MDVR and CWR22Rv1 cells were treated with different doses of ARVibs for 16 h and whole-cell lysates were collected and subjected to western blot. D CWR22Rv1 cells were treated with enzalutamide with or without ARVibs (#1, #34, #7, and #31), total cell numbers were determined at 0, 3, 5 days. E The CDI of enzalutamide or abiraterone with ARVibs in CWR22Rv1 and C4-2B MDVR cells were calculated. *p < 0.05. Results are the mean of three independent experiments (±S.D.). AR-FL: full-length AR, AR-Vs AR-Variants, Enza enzalutamide, Abi abiraterone, Nic niclosamide, CDI: coefficient of drug interaction.
