Synthesis and cytotoxic activity evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines

Molecules. 2014 Aug 12;19(8):12048-64. doi: 10.3390/molecules190812048.

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 9 and 15 exhibited strong cytotoxic activities against LNCaP cells (IC50<5 μM), and compound 8 (IC50=8.25 μM) possessed the most potent activity against DU145 cells. However, these compounds also exhibited cytotoxicity towards 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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Male
  • Piperazine
  • Piperazines / administration & dosage*
  • Piperazines / chemical synthesis*
  • Piperazines / chemistry
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / pathology
  • Structure-Activity Relationship

Substances

  • Piperazines
  • Piperazine