一些新型白藜芦醇酰胺衍生物的合成及生物评价作为潜在的抗肿瘤药物。
Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.
机构信息
School of Medical Engineering, Hefei University of Technology, Hefei, PR China.
出版信息
Eur J Med Chem. 2013 Apr;62:222-31. doi: 10.1016/j.ejmech.2012.11.021. Epub 2012 Nov 20.
Three series of novel resveratrol amide derivatives (1a-q, 2a-h, 3a-l) were synthesized and evaluated for their biological activities. All compounds were characterized by (1)H NMR, (13)C NMR, MS and elemental analysis. Furthermore, compound 3e was also characterized by X-ray crystallography. All the compounds were evaluated for their anti-tumor activity against MCF-7, A549 and B16-F10 tumor cell lines as well as cyclooxygenase-2 (COX-2)-derived prostaglandin E2 (PGE2) inhibitory activity of murine macrophage RAW 264.7 cell line. Among them, compounds 1c, 1g and 3e displayed the most potent COX-2 inhibitory activity with the IC50 values of 1.02, 1.27 and 1.98 μM, respectively. Molecular docking studies were performed to position compounds 1c and 3e into the active site of COX-2 to determine the probable binding modes.
合成了三个系列的新型白藜芦醇酰胺衍生物（1a-q、2a-h、3a-l），并对其生物活性进行了评价。所有化合物均通过 1H NMR、13C NMR、MS 和元素分析进行了表征。此外，化合物 3e 还通过 X 射线晶体学进行了表征。所有化合物均对 MCF-7、A549 和 B16-F10 肿瘤细胞系的抗肿瘤活性以及小鼠巨噬细胞 RAW 264.7 细胞系中环氧化酶-2（COX-2）衍生的前列腺素 E2（PGE2）抑制活性进行了评价。其中，化合物 1c、1g 和 3e 对 COX-2 的抑制活性最强，IC50 值分别为 1.02、1.27 和 1.98 μM。进行了分子对接研究，以将化合物 1c 和 3e 定位到 COX-2 的活性部位，以确定可能的结合模式。
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