Secondary Logo

Journal Logo

Institutional members access full text with Ovid®

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

Guo, Guangzhu; Liu, Jianzhen; Wang, Guanjie; Zhang, Daoguang; Lu, Jinjie; Zhao, Guisen

doi: 10.1097/CAD.0000000000000322
PRECLINICAL REPORTS
Buy

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.

Key Laboratory of Chemical Biology, Ministry of Education, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, People’s Republic of China

* Guangzhu Guo and Jianzhen Liu contributed equally to the writing of this article.

Correspondence to Guisen Zhao, PhD, Key Laboratory of Chemical Biology, Ministry of Education, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, Shandong, China Tel/fax: +86 531 8838 2009; e-mail: guisenzhao@sdu.edu.cn

Received September 29, 2015

Accepted November 4, 2015

Copyright © 2016 Wolters Kluwer Health, Inc. All rights reserved.