【摘要】 目的设计合成β-榄香烯芳杂环衍生物,并进行体外抗癌活性筛选。方法以β-榄香烯为起始原料,经烯丙位的氯代反应,合成β-榄香烯氯代物,再通过亲核取代反应在β-榄香烯母体上引入含氮芳杂环合成目标化合物。采用SRB法测定目标化合物对癌细胞增殖的抑制作用。结果共合成9个未见报道的β-榄香烯类化合物,其结构经红外光谱、核磁共振氢谱和质谱确证。所有化合物对3种人癌细胞HL-60、HeLa、SGC-7901的IC50值均远低于β-榄香烯。结论在β-榄香烯结构中引入含氮芳杂环,可改善化合物的水溶性,显著提高体外抗癌活性。更多还原

【Abstract】 Aim To design and synthesize some novel aromatic heterocycles derivatives of β-elemene and eva-(luate) their antitumor activity to find better β-elemene derivatives with antitumor activities.Methods The target compounds were synthesized from β-elemene via chlorination and nucleophilic substitution.Their effects on growth inhibition against HL-60,HeLa and SGC-7901 cells were determined by SRB assay.Results Nine compounds that had not been reported were synthesized and their structures were confirmed by IR,()~1H-NMR and MS.All the compounds had significantly higher anti-proliferative activities than β-elemene.Conclusion An introduction of aromatic heterocycles with nitrogen into the skeleton of β-elemene would increase antitumor activity.更多还原