白藜芦醇类似物的合成与抗肿瘤活性

Synthesis and Anti-tumor Activity of Resveratrol Analogues

为了寻找抗肿瘤候选化合物,根据生物电子n b等排原理,设计合成系列白藜芦醇类似物。以芳香杂环醛和取代甲苯为起始原料,经缩合、脱甲基化反应得标题化合物。通过IR、~1HNMR和^(13)CNMR对目标化合物进行结构确定。采用MTT法对合成的化合物进行体外抗肿瘤活性评价。结果表明,化合物对所测肿瘤细胞有不同的增殖抑制作用,其中E-(2-呋喃)(3,5-二羟基苯基)乙烯、E-(2-吡咯)(3,5-二羟基苯基)乙烯的抗肿瘤活性较突出,高于对照物白藜芦醇,值得进一步研究。

To obtain anti-tumor candidate compounds,some resveratrol analogues were designed via bioisosterism method. The target compounds were synthesized using aromatic aldehyde and substituted toluene as starting materials via condensation,demethylation. The structures of all the compounds were confirmed by IR,~1HNMR and ^（13）CNMR. The anti-tumor activities of the target compounds were evaluated against two different tumor cell lines by an MTT assay. The result indicated that they exhibited certain anti-tumor activities,and compounds E-（ 2-fural）（ 3,5-dihydroxyphenyl） ethane and E-（ 2-pyrrole）（ 3,5-dihydroxyphenyl） ethane showed better anti-tumor activity against A-549 and SGC-7901 than the positive drug resveratrol,which were worth to further investigating.