School of Medical Engineering, Hefei University of Technology, Hefei 230009, PR China.
Bioorg Med Chem. 2012 Jan 15;20(2):1113-21. doi: 10.1016/j.bmc.2011.11.017. Epub 2011 Dec 1.
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.
一系列具有姜黄素部分的白藜芦醇衍生物被合成,并评价它们对三种癌细胞系(包括鼠黑色素瘤 B16-F10、人肝癌 HepG2 和人肺癌 A549)的体外增殖活性。其中,化合物 C5 对 B16-F10 的体外增殖活性最强,IC50 值为 0.71μg/mL。化合物 C5 对微管蛋白聚合也表现出良好的抑制活性,IC50 值为 1.45μg/mL。此外,还进行了对接模拟,将 C5 定位到微管蛋白-秋水仙素结合位点,以确定可能的结合模式。