吲哚螺吡咯类衍生物的合成及其抗肿瘤细胞活性筛选﹡

摘要

目的：合成一类螺环结构的4′－芳基－3′－吡啶甲酰基螺[吲哚－3，2′－吡咯啉]－2－酮化合物，并对其抗肿瘤细胞活性进行初步筛选。方法利用多组分反应方法合成吲哚螺环化合物，并采用四甲基偶氮唑盐比色（ MTT）法测试其细胞活性。结果反应在2～3 h内完成，产率80％～85％，产物通过光谱数据表征确认结构；并筛选了其对肝癌细胞BEL－7402、人低分化胃癌细胞BGC－823、人乳腺癌细胞MDA－MB－231的抑制活性。结论螺[吲哚－3，2′－吡咯啉]类化合物含多个活性杂环骨架，有潜在的抗肿瘤细胞活性作用。%Objectives To synthesis spiro[indoline-3,2′-pyrrolidin] derivatives and investigate their anticancer activities .Methods The target compounds were synthesized via multi -component reactions ,and evaluated for their an-ticancer activities against human cancer cell lines by MTT assay .Rseults The reaction was completed within 2-3 hours with yields of 80%-85%.The structures of the products were determined by IR , 1 H NMR spectra, and the anticancer activities against human cancer cell lines BEL -7402, BGC-823 and MDA-MB-231 were tested.Conclusion The spiro[indoline-3,2′-pyrrolidin] derivatives contain muti -heterocyclic skeletons which are expected to exhibit poten-tial biological activities .