目的合成β-榄香烯胺类衍生物,并对其体外抗癌活性进行初步的评价。方法β-榄香烯经氯代、胺化制备目标化合物。以SRB法测试目标化合物对HL-60、HeLa、SGC-7901细胞的增殖抑制活性。结果与结论合成了12个新化合物,其结构经IR、MS和1H-NMR确证。初步药理结果显示大部分目标化合物的体外抗癌活性明显强于β-榄香烯。 Objective To synthesize β-elemene derivatives and evaluate their antitumor activity in vitro. Methods β-Elemene chloride, amination to prepare the target compound. The inhibitory activity of the target compound on the proliferation of HL-60, HeLa and SGC-7901 cells was tested by SRB method. Results and Conclusion Twelve novel compounds were synthesized and their structures were confirmed by IR, MS and 1H-NMR. Preliminary pharmacological results show that most of the target compounds in vitro anticancer activity was significantly stronger than β-elemene.