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. Epub 2014 Nov 26.

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.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects*
  • Drug Design*
  • Drug Screening Assays, Antitumor
  • Humans
  • Male
  • Models, Molecular
  • Molecular Structure
  • Piperazines / chemical synthesis*
  • Piperazines / pharmacology*
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / pathology
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Piperazines