Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 28, Issue 23-24, Pages 3634-3638Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.10.037
Keywords
Cinnamic acid; Sulfonamide; Antiproliferative activity; Molecular docking; Anti-tubulin polymerization
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Funding
- China Postdoctoral Science Foundation [2014M551563]
- International Postdoctoral Exchange Fellowship Program [20130023]
- National Natural Science Foundation of China [81701164]
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A new series of novel cinnamic acyl sulfonamide derivatives were designed and synthesized and evaluated their anti-tubulin polymerization activities and anticancer activities. One of these compounds, compound 5a with a benzdioxan group, was observed to be an excellent tubulin inhibitor (IC50 = 0.88 mu M) and display the best antiproliferative activity against MCF-7 with an IC50 value of 0.17 mu g/mL. Docking simulation was performed to insert compound 5a into the crystal structure of tubulin at colchicine binding site to determine the probable binding model. 3D-QSAR model was also built to provide more pharmacophore understanding that could be used to design new agents with more potent anti-tubulin polymerization activity.
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