Synthesis, biological evaluation and molecular docking studies of resveratrol derivatives possessing curcumin moiety as potent antitubulin agents |
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Authors: | Ruan Ban-Feng Lu Xiang Li Ting-Ting Tang Jian-Feng Wei Yao Wang Xiao-Liang Zheng Shi-Li Yao Ri-Sheng Zhu Hai-Liang |
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Institution: | School of Medical Engineering, Hefei University of Technology, Hefei 230009, PR China. |
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Abstract: | A series of resveratrol derivatives possessing curcumin moiety were synthesized and evaluated for their antiproliferative activity against three cancer cell lines including murine melanoma B16-F10, human hepatoma HepG2 and human lung carcinoma A549. Among them, compound C5 displayed the most potent in vitro antiproliferative activity against B16-F10 with IC(50) value of 0.71 μg/mL. Compound C5 also exhibited good tubulin polymerization inhibitory activity with IC(50) value of 1.45 μg/mL. Furthermore, docking simulation was carried out to position C5 into the tubulin-colchicine binding site to determine the probable binding mode. |
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