2. Academic Validation
  3. Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines

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

Affiliations

  • 1 Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
  • 2 Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China. Electronic address: mryuanmu838@sina.com.
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.

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