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Synthesis and Biological Evaluation of Arylpiperazine Derivatives as Anticancer Agents

[ Vol. 15 , Issue. 11 ]

Author(s):

Hong Chen, Zonglin Yang, Tao Sun, Jiangxiu Niu, Xiumei Tian* and Mu Yuan*   Pages 981 - 989 ( 9 )

Abstract:


Prostate cancer is the most common malignancy in men. For the development of potential anti-prostate cancer agents, a series of arylpiperazine derivatives was synthesized based on previous studies. The target compounds were synthesized via three-step reaction and their in vitro cytotoxic efficacies against a panel of three human prostate cancer cell lines (PC-3, LNCaP, and DU145) and one normal prostate epithelial cell line (WPMY-1) were evaluated by CCK-8 assay. The derivatives 6, 7, 8, 10, 11, 13, 16, 20, 21, 22 and 25 showed important cytotoxic actions against the individual tested cancer cell line with IC50 values <10 μM. The results showed that the o-substituted phenyl group derivatives and m-substituted phenyl group derivatives displayed improved cytotoxic activity against PC-3 cells.

Keywords:

Synthesis, derivatives, prostate cancer, CCK-8 assay, cytotoxicity, structure-activity relationship.

Affiliation:

College of Food and Drug, Luoyang Normal University, Luoyang, Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou, College of Food and Drug, Luoyang Normal University, Luoyang, College of Food and Drug, Luoyang Normal University, Luoyang, School of Basic Medical Sciences, Guangzhou Medical University, Guangzhou, Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou

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