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目的合成系列新型N-芳基-α-氧代苯乙酰胺类化合物,测定体外抗增殖活性。方法引入分子对接研究讨论该类化合物在微管蛋白秋水仙碱位点的结合方式;以3,4,5-三甲氧基苯甲醛为原料,经二氯卡宾插入反应完成中间体3,4,5-三甲氧基α-羟基苯乙酸的制备,再经酰胺化、脱苄基、PCC氧化等步骤制得目标化合物;以阿霉素为阳性对照药,采用MTT法测定目标化合物对肿瘤细胞株HT-1080和KB的抗增殖活性。结果与结论合成了20个未见文献报道的化合物,其结构经MS、1H-NMR确证;活性测试结果表明,6个化合物表现出较好的抗增殖活性。
AIM: To synthesize a series of novel N-aryl-α-oxoacetamide compounds for the determination of anti-proliferative activity in vitro. Methods The molecular docking was introduced to study the binding mode of these compounds at the tubulin colchicine site. 3,4,5-trimethoxybenzaldehyde was used as the starting material and inserted through the reaction of dichlorocarbene to complete the intermediates 3,4. 5-trimethoxy-α-hydroxyphenylacetic acid, followed by amidation, debenzylation, PCC oxidation and other steps to obtain the target compound; doxorubicin as a positive control drug, using MTT assay of the target compound on tumor cell lines HT-1080 and KB antiproliferative activity. RESULTS AND CONCLUSION: Twenty non-reported compounds were synthesized and their structures were confirmed by MS and 1H-NMR. The activity test results showed that the six compounds showed good anti-proliferative activity.