Here, we identified two specific inhibitors of AR/p52 interaction, AR/p52-01 and AR/p52-02, that are capable of inhibiting the growth of both parental androgen-dependent LNCaP and its castration-resistant C4-2 variant human prostate carcinoma cell lines under androgen-deprived conditions with IC50 values less than 10 μM. This evidence concerns the gene AR and prostate carcinoma.