期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 26, 期 1, 页码 8-16出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.09.019
关键词
Anti-tumor activity; Chalcone; Cat L; Cat K
资金
- National Natural Science Foundation of China [81473097]
- Student Fund of Innovation Project of Peking Union Medical College [2015-1007-22]
- CAMS initiative for Innovative Medicine [2016-I2M-3-022]
A series of chalcone derivatives bearing benzamide or benzenesulfonamide moieties were synthesized and evaluated for their anti-tumor effect on HCT116, MCF7 and 143B cell lines in vitro. SAR analysis showed that compounds bearing a benzenesulfonamide group had greater potency than those bearing a benzamide group. It was also shown that compounds with a mono-methyl or mono-halogen group at the 3-position on the terminal phenyl ring were more effective than those with trifluoromethyl or methoxy groups. Compound 8e exhibited the most potent anti-tumor activities against HCT116, MCF7 and 143B cell lines, with IC50 values of 0.597, 0.886 and 0.791 mu M, respectively. Molecular docking studies and enzymatic assays demonstrated that the anti-tumor activity of compound 8e might be regulated by Cat L and Cat K. (C) 2017 Elsevier Ltd. All rights reserved.
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