LAUSR

BACKGROUND The androgen receptor (AR) signaling functions is a critical driving force for the progression of prostate cancer (PCa) to bring about anti-prostate cancer agents, and AR has been proved to be an effective therapeutic target even for castration-resistant prostate cancer (CRPC). OBJECTIVE In order to discover novel anti prostate cancer agents, we performed structural modifications based on the lead compounds T3 and 10e. METHODS A set of 1-methyl- 1H-pyrazole-5-carboxamide derivatives were synthesized and evaluated for their inhibitory activities against both expressions of prostate-specific antigen(PSA) and growth of PCa cell lines. RESULTS Compound H24 was found to be able to completely block PSA expression at 10 µM, and showed prominent antiproliferative activity in both the LNCaP cell line (GI 50 = 7.73 µM) and PC-3 cell line (GI 50 = 7.07 µM). CONCLUSIONS These preliminary data supported a further evaluation of compound H24 as a potential agent to treat prostate cancer.