Journal
BIOORGANIC CHEMISTRY
Volume 78, Issue -, Pages 332-340Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.03.028
Keywords
Chalcone; Tubulin; Anticancer activity; Claisen-Schmidt condensation; Naphthalene
Funding
- National Natural Science Foundation of China [81660574]
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A series of aminochalcone derivatives have been synthesized, characterized by HRMS, H-1 NMR and C-13 NMR and evaluated for their antiproliferative activity against HepG2 and HCT116 human cancer cell lines. The most of new synthesized compounds displayed moderate to potent antiproliferative activity against test cancer cell lines. Among the derivatives, compound 4 displayed potent inhibitory activity with IC50 values ranged from 0.018 to 5.33 mu M against all tested cancer cell lines including drug resistant HCT-8/T. Furthermore, this compound showed low cytotoxicity on normal human cell lines (LO2). The in vitro tubulin polymerization assay showed that compound 4 inhibited tubulin assembly in a concentration-dependent manner with IC50 value of 7.1 mu M, when compared to standard colchicine (IC50 = 9.0 mu M). Further biological evaluations revealed that compound 4 was able to arrest the cell cycle in G2/M phase. Molecular docking study demonstrated the interaction of compound 4 at the colchicine binding site of tubulin. All the results indicated that compound 4 is a promising inhibitor of tubulin polymerization for the treatment of cancer. (C) 2018 Elsevier Inc. All rights reserved.
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