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Molecules 2017, 22(11), 1857; doi:10.3390/molecules22111857

Synthesis and Antitumor Activity of Novel Arylpiperazine Derivatives Containing the Saccharin Moiety

1,* and 2,*
College of Food and Drug, Luoyang Normal University, 6# Jiqing Road, Luoyang 471934, China
Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 511436, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 20 September 2017 / Revised: 17 October 2017 / Accepted: 25 October 2017 / Published: 29 October 2017
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Prostate cancer is a major public health problem worldwide. For the development of potential anti-prostate cancer agents, a series of novel arylpiperazine derivatives containing the saccharin moiety based on previous studies was designed, synthesized, and evaluated in prostate (PC-3, LNCaP, and DU145) cancer cell lines for their anticancer activities. The majority of the compounds exhibited excellent selective activity for the tested cancer cells. Compounds 4 and 12 exhibited strong cytotoxic activities against DU145 cells (half maximal inhibitory concentration (IC50) < 2 μM). The structure–activity relationship (SAR) of these arylpiperazine derivatives was also discussed based on the obtained experimental data. This work provides a potential lead compound for anticancer agent development focusing on prostate cancer therapy. View Full-Text
Keywords: synthesis; arylpiperazine derivatives; cytotoxic activity; CCK-8; structure-activity relationship synthesis; arylpiperazine derivatives; cytotoxic activity; CCK-8; structure-activity relationship

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Chen, H.; Xu, B.-B.; Sun, T.; Zhou, Z.; Ya, H.-Y.; Yuan, M. Synthesis and Antitumor Activity of Novel Arylpiperazine Derivatives Containing the Saccharin Moiety. Molecules 2017, 22, 1857.

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