A new series of 5-[ (lH-indol-3-yl) methylene] thiazolidine-2,4-dione derivatives(el-e9)were synthesized by incorporating different N-substituted-lH-indole into thiazolidine-2,4-dione with methylene bond,and further modified at the nitrogen of thia-zolidine-2,4-dione by different groups. Their structures were determined by IR.1H NMR and HRMS. Their antitumor activity was e-valuated over five cancer cells by the MTT assay. All the target compounds displayed antitumor activity against A549.HCT116 and PC-9,and those with benzyl at 1-position of indole(el and e3)had similar anticancer activity as 5-Fluorouracil(5-FU)over the test cancer cells (exception of A375) ,and had higher activity against A549 and HCT116(IC50 value lower than 30 μM) providing a good lead for subsequent optimization as cancer inhibitory agents.%将N-取代吲哚-3-甲醛和2,4-噻唑烷二酮通过亚甲基键合,再对噻唑烷二酮氮取代,合成了一系列5-(3-吲哚基)亚甲基噻唑烷-2,4-二酮衍生物(e1-e9).采用IR,1H NMR和HRMS对其结构进行了表征；采用MTT法对目标物抑制5种癌细胞增殖活性进行了测试.结果表明,所有目标物对A549、HCT116和PC-9表现出抑制活性,其中吲哚氮被苄基取代的化合物e1和e3对测定的癌细胞增殖抑制活性与5-氟尿嘧啶(5-FU)相近,并且对A549和HCT116表现出中等的抑制活性(IC50 ＜30 μM).
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