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以取代靛红,(E)-硝基异噁唑芳烯烃和苯基甘氨酸为原料,乙腈为溶剂,经1,3-偶极子3+2环加成反应合成了8个新型的异噁唑拼接吡咯螺环氧化吲哚化合物(3a~3h),产率41%~62%,d/r值为2∶1~10∶1,其结构经~1H NMR,~(13)C NMR和HR-ESI-MS表征。采用MTT法研究了3a~3h对人肺癌细胞(A549),人前列腺(PC-3)和人白血病细胞(K562)的体外抗肿瘤活性。结果表明:3a,3b和3c分别对K562,PC-3和A549具有较好的抑制活性,其对应的IC50为16.0μmol·L~(-1),21.2μmol·L~(-1)和24.4μmol·L~(-1),优于顺铂(26.1μmol·L~(-1),27.2μmol·L~(-1)和25.6μmol·L~(-1))。
In this study, 8 new kinds of heterotrophic compounds were synthesized by the 3 + dipolar 3 + 2 cycloaddition reaction using isatin, (E) -nitroisoxazole and phenylglycine as raw materials and acetonitrile as solvent Pyrazole spiro pyrrole spiro epoxy compounds (3a ~ 3h), the yield of 41% to 62%, d / r value of 2: 1 to 10: 1, the structure of ~ 1H NMR, And HR-ESI-MS. In vitro anti-tumor activity of human lung cancer cells (A549), human prostate (PC-3) and human leukemia cells (K562) were studied by MTT assay. The results showed that 3a, 3b and 3c had good inhibitory activity on K562, PC-3 and A549, respectively. The corresponding IC50 values were 16.0μmol·L -1, 21.2μmol·L -1 and 24.4 μmol·L -1, which was better than that of cisplatin (26.1μmol·L -1, 27.2μmol·L -1 and 25.6μmol·L -1).