Journal
BIOORGANIC CHEMISTRY
Volume 103, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.104141
Keywords
Pyrazole; Naphthalene; Anticancer; Tubulin polymerization inhibitor
Funding
- National Natural Science Foundation of China [81660574]
- One Thousand Talents Program of Guizhou Province (the fifth group) [[2019]4]
- Guizhou Provincial Natural Science Foundation [[2019]1256]
- Doctor Foundation of Guizhou Medical University [[2018]004]
- Science and Technology Fund of Guizhou Health Commission [gzwjkj2019-1-183]
- Guizhou Science and Technology Department [[2016]5613\5677, [2017]5601]
- Local Science and Technology Project Guided by Central Administration [[2018]4006]
- Guiyang Science and Technology Bureau [[2017]30-29]
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A new series of pyrazole-naphthalene derivatives (5a-5q) have been synthesized and evaluated for their anticancer activity against human breast cancer cell lines (MCF-7). Most of newly synthesized compounds (except 5i, 5m, and 5p) exhibited potent antiproliferative activity in the range of IC50 = 2.78 +/- 0.24 mu M - 9.13 +/- 0.47 mu M. Among them, compound 5j (IC50 = 2.78 +/- 0.24 mu M), bearing ethoxy at the 4-position of the phenyl ring, was found to be the most active compound in this series of compounds, with five folds more active than the standard drug cisplatin (IC50 = 15.24 +/- 1.27 mu M). In addition, compound 5j and colchicine showed the same ability to inhibit tubulin polymerization with the IC50 values of 4.6 mu M and 6.7 mu M, respectively. Cellular mechanism studies elucidated that compound 5j arrested the cell cycle at G2/M phase and induced apoptosis. Furthermore, molecular docking analysis revealed that compound 5j formed stable interactions in the colchicine-binding site of tubulin.
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