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以取代靛红和肌氨酸为原料制得1,3-偶极子,再与(E)-芳姜烯酮类化合物在乙腈中经3+2环加成反应合成了10个新型的芳姜黄酮拼合吡咯螺环氧化吲哚类化合物(3a~3j),产率70%~91%,d/r值15∶1~>20∶1,其结构经~1H NMR,~(13)C NMR和HR-MS(ESI-TOF)表征。采用MTT法研究了3a~3j对人肺癌细胞(A549)和人白血病细胞(K562)的体外抗肿瘤活性。结果表明:3f对K562抑制活性较好(IC50=31.1μmol·L-1),3b对A549抑制活性较好(IC50=54.1μmol·L~(-1))。
The 1,3-dipole was obtained from the substituted isatin and sarcosine, and then 10 new aromatic compounds were synthesized via 3 + 2 cycloaddition with (E) -aroquinone in acetonitrile (3a ~ 3j), the yield was 70% ~ 91% and the d / r was 15:1 ~> 20:1. The structure of the compounds was confirmed by ~ 1H NMR, C NMR and HR-MS (ESI-TOF) characterization. In vitro anti-tumor activity of 3a ~ 3j against human lung cancer cells (A549) and human leukemia cells (K562) was studied by MTT assay. The results showed that 3f had better inhibitory activity on K562 (IC50 = 31.1μmol·L-1) and 3b on A549 (IC50 = 54.1μmol·L -1).