A novel series of 3-(4-fluorophenyl)-1H-pyrazole derivatives were synthesized and evaluated for their antiproliferative activity against two prostate cancer cell lines (LNCaP and PC-3) and androgen receptor target gene prostate-specific antigen (PSA) inhibitory activity in LNCaP cells.
Several compounds showed potent antiproliferative activity against LNCaP cells and showed a promising PSA downregulation rate. Among these, compound 10e selectively inhibited LNCaP cell growth with an IC50 value of 18 μmol/l and showed a PSA downregulation rate of 46%, which was better than the lead compound T3.
Anti-cancer drugs. 2015 Dec 03 [Epub ahead of print]
Guangzhu Guo, Jianzhen Liu, Guanjie Wang, Daoguang Zhang, Jinjie Lu, Guisen Zhao
Key Laboratory of Chemical Biology, Ministry of Education, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, People's Republic of China.