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Letters in Organic Chemistry


ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

Research Article

Synthesis and Biological Evaluation of Arylpiperazine Derivatives as Anticancer Agents

Author(s): Hong Chen, Zonglin Yang, Tao Sun, Jiangxiu Niu, Xiumei Tian* and Mu Yuan*

Volume 15 , Issue 11 , 2018

Page: [981 - 989] Pages: 9

DOI: 10.2174/1570178615666180518103641

Price: $65


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.

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