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

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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 8, 10, 13, 17 and 20 exhibited strong cytotoxic activities against the tested cancer cell lines (IC50 <3 μmol/L). In addition, these compounds exhibited weak cytotoxic effects on human epithelial prostate normal cells WPMY-1. The structure–activity relationship (SAR) of these arylpiperazine derivatives was also discussed based on the obtained experimental data.

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Chen, H., Xu, F., Xu, B. B., Xu, J. Y., Shao, B. H., Huang, B. Y., & Yuan, M. (2016). Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines. Chinese Chemical Letters, 27(2), 277–282. https://doi.org/10.1016/j.cclet.2015.09.016

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