Synthesis and biological evaluation of 3-(4-fluorophenyl)-1H-pyrazole derivatives as androgen receptor antagonists. Issue 4 (April 2016)

• Record Type: Journal Article
• Authors: Guo, Guangzhu; Liu, Jianzhen; Wang, Guanjie; Zhang, Daoguang; Lu, Jinjie; Zhao, Guisen
• Is Part Of: Anti-cancer drugs. Volume 27:Issue 4(2016)
• Publication Date: 2016-04
• Subjects: androgen receptor -- antagonist -- prostate cancer -- pyrazole derivatives; Antineoplastic agents -- Periodicals; Cancer -- Chemotherapy -- Periodicals; Antineoplastic Agents -- therapeutic use -- Periodicals; Drug Therapy -- Periodicals; 616.994061
• DOI: 10.1097/CAD.0000000000000322
• Languages: English
• ISSNs: 0959-4973

Abstract

Abstract : A novel series of 3-(4-fluorophenyl)-1 H -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, compound10e 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 compoundT3 .