期刊
MOLECULES
卷 22, 期 11, 页码 -出版社
MDPI
DOI: 10.3390/molecules22111857
关键词
synthesis; arylpiperazine derivatives; cytotoxic activity; CCK-8; structure-activity relationship
资金
- Natural Science Foundation of China [21705072]
- Henan Province Science and Technology Attack Plan Foundation [162102310477, 172102310478]
- Key Scientific Research Project of Higher Education of Henan Province [16A350008, 17A150039, 17B350001]
- National Scientific Research Foundation of Luoyang Normal University [2015-PYJJ-005]
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 M). 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.
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