Chen Hong, Xu Fang, Liang Xue, Xu Bing-Bing, Yang Zong-Lin, He Xue-Lan, Huang Bi-Yun, Yuan Mu
Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
Bioorg Med Chem Lett. 2015 Jan 15;25(2):285-7. doi: 10.1016/j.bmcl.2014.11.049. Epub 2014 Nov 26.
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.
合成了一系列新型芳基哌嗪衍生物。通过CCK-8法评估了所有合成化合物对三种人前列腺癌细胞系（PC-3、LNCaP和DU145）的体外细胞毒活性。化合物10、24和29对LNCaP细胞表现出较强的细胞毒活性（IC50<3μM）。此外，这些化合物对人前列腺上皮正常细胞RWPE-1表现出较弱的细胞毒作用。还根据获得的实验数据讨论了这些芳基哌嗪衍生物的构效关系（SAR）。
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