期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 6, 页码 806-810出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.01.025
关键词
2-Benzoylbenzofuran; Anticancer activity; Cytotoxicity; Apoptosis
资金
- Natural Science Foundation of China [81560620, 81460624]
- Yunnan Provincial Science and Technology Department-Applied Basic Research Joint Special Funds of Yunnan University of Traditional Chinese Medicine [2017FF117(-023), 2016FA037]
- Construction project funding of university key laboratories in Yunnan province
- Yunnan science and Technology Office [2018FY001-001]
- Yunnan University [2018FY001-001]
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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