吲哚螺吡咯类衍生物的合成及其抗肿瘤细胞活性筛选

Spiro [ indoline - 3,2＇ - pyrrolidin ] derivatives： synthesis and the screening of anticancer activity

目的合成一类螺环结构的4’-芳基-3’-吡啶甲酰基螺[吲噪-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（MTr）法测试其细胞活性。结果反应在2-3h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＇ -pyrrolidinj 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 MTY assay. Results The reaction was completed within 2 - 3 hours with yields of 80% -85%. The structures of the products were determined by IR, 1H 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 -heterocyelic skeletons which are expected to exhibit poten- tial biological activities.