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目的设计合成β-榄香烯吲哚衍生物并进行体外抗癌活性筛选。方法通过合成β-榄香烯氯代物,在其结构中引入3-吲哚乙胺结构片段进而合成β-榄香烯吲哚衍生物。采用MTT法测定目标化合物对K562白血病细胞的增殖抑制作用。结果合成了15个未见文献报道的β-榄香烯吲哚衍生物。目标化合物的结构经1H-NMR、MS谱确证。活性实验结果显示14个目标化合物的活性高于β-榄香烯。结论在β-榄香烯结构中引入3-吲哚乙胺结构片段有利于提高此类化合物的抗癌活性。
OBJECTIVE To design and synthesize β-elemene indole derivatives for screening in vitro anticancer activity. Methods By synthesizing β-elemene chloride, 3-indole ethylamine structure fragment was introduced into its structure to synthesize β-elemene indole derivatives. The inhibitory effect of the target compound on the proliferation of K562 leukemia cells was determined by MTT assay. Results Fifteen β-elemene indole derivatives were synthesized. The structure of the target compound was confirmed by 1H-NMR and MS. The activity test results showed that the 14 target compounds were more active than β-elemene. Conclusion The introduction of 3-indole ethylamine moiety into the β-elemene structure is helpful to improve the anticancer activity of these compounds.