2-Benzoylbenzofuran derivatives possessing piperazine linker as anticancer agents |
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Authors: | Hui Gao Xia Zhang Xiao-Jia Pu Xi Zheng Bei Liu Gao-Xiong Rao Chun-Ping Wan Ze-Wei Mao |
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Institution: | 1. College of Pharmaceutical Science, Yunnan University of Traditional Chinese Medicine, Kunming 650500, PR China;2. Central Laboratory, The NO. 1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021, PR China |
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Abstract: | A series of novel 2-benzoylbenzofuran derivatives possessing piperazine linker have been prepared, and their in vitro anticancer activity against a panel of human tumor cell lines by MTT assay were evaluated. The results demonstrated that tertiary amine derivatives exhibited better cytotoxic activity, and SAR study revealed that electron-donating substituents on the phenyl ring of the derivatization functionality contributed to potent anticancer activities. Among them, compounds 6, 9, 11, 18, 23 and 25 displayed both better anti-tumor activity and lower cytotoxic effect on human normal liver cell L02. Further apoptosis analysis showed that compound 18 significantly induced apoptosis in A549 cell, which was considered as the most potent anticancer agent. |
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Keywords: | 2-Benzoylbenzofuran Anticancer activity Cytotoxicity Apoptosis |
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