Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines

  • Bioorg Med Chem Lett. 2015 Jan 15;25(2):285-7. doi: 10.1016/j.bmcl.2014.11.049.
Hong Chen  1 ,  Fang Xu  1 ,  Xue Liang  1 ,  Bing-Bing Xu  1 ,  Zong-Lin Yang  1 ,  Xue-Lan He  1 ,  Bi-Yun Huang  1 ,  Mu Yuan  2
Affiliations
  • 1. Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
  • 2. Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China. Electronic address: [email protected].
PMID: 25488843 DOI: 10.1016/j.bmcl.2014.11.049
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. Compounds 10, 24 and 29 exhibited strong cytotoxic activities against LNCaP cells (IC50 <3μM). 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.

Keywords
Arylpiperazine derivatives; CCK-8; Cytotoxic activity; Structure–activity relationship; Synthesis.