Citation: Hong Chen, Fang Xu, Bing-Bing Xu, Jing-Yi Xu, Bin-Hao Shao, Bi-Yun Huang, Mu Yuan. Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines[J]. Chinese Chemical Letters, ;2016, 27(02): 277-282. doi: 10.1016/j.cclet.2015.09.016 shu

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

Hong Chen ^a,b ,
Fang Xu ^b ,
Bing-Bing Xu ^b ,
Jing-Yi Xu ^b ,
Bin-Hao Shao ^b ,
Bi-Yun Huang ^b ,
Mu Yuan ^b,,

a.
a. College of Chemistry and Chemical Engineering, Luoyang Normal University, Luoyang 471022, China;
b.
b. Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China

Corresponding author: Mu Yuan,
Received Date: 7 April 2015
Available Online: 9 June 2015
Fund Project: the China Postdoctoral Science Foundation (Nos. 2013M542165, 2013M531837) (No. cx2d1127) the National Science Foundation of Guangdong Province (No. S2013040014088) (Nos. 2013M542165, 2013M531837)the Guangzhou Postdoctoral Scientific Research Foundation (Nos. Q130, Q074). (No. S2013040014088)

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.
- Synthesis,
- Arylpiperazine derivatives,
- Cytotoxic activity,
- CCK-8,
- Structure-activity relationship
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