Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines. Issue 2 (15th January 2015)

• Record Type: Journal Article
• Authors: Chen, Hong; Xu, Fang; Liang, Xue; Xu, Bing-Bing; Yang, Zong-Lin; He, Xue-Lan; Huang, Bi-Yun; Yuan, Mu
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 2(2015)
• Page Start: 285
• Page End: 287
• Publication Date: 2015-01-15
• Subjects: Synthesis -- Arylpiperazine derivatives -- Cytotoxic activity -- CCK-8 -- Structure–activity relationship; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2014.11.049
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of novel arylpiperazine derivatives was synthesized. The in vitro cytotoxic activities of all synthesized compounds against three human prostate cancer cell lines (PC-3, LNCaP, and DU145) were evaluated by a CCK-8 assay. Compounds10, 24 and29 exhibited strong cytotoxic activities against LNCaP cells (IC50 <3 μM). In addition, these compounds exhibited weak cytotoxic effects on human epithelial prostate normal cells RWPE-1. The structure–activity relationship (SAR) of these arylpiperazine derivatives was also discussed based on the obtained experimental data.