Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 26, Issue 1, Pages 8-16Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.09.019
Keywords
Anti-tumor activity; Chalcone; Cat L; Cat K
Funding
- 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]
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available