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合成了系列新的3-芳基噻唑烷-4-酮-2-酰胺衍生物,并测试了化合物抑制肿瘤细胞增殖活性.部分化合物对A-549和Hela肿瘤细胞有弱的细胞毒性,而对BGC-823没有抑制作用,表现出一定的选择性.其中,化合物7ad对A-549有较强的抑制活性(IC50=21.0μmol·L-1),与阳性对照顺铂的抑制活性(IC50=19.4μmol·L-1)相当.初步的构效关系表明化合物的立体结构可能对其抗肿瘤活性影响较大.
A series of novel 3-arylthiazolidin-4-one-2-carboxamide derivatives were synthesized and tested for their ability to inhibit the proliferation of tumor cells.Part of compounds has weak cytotoxicity on A-549 and Hela tumor cells, BGC-823 had no inhibitory effect, showing a certain selectivity, among which compound 7ad had stronger inhibitory activity on A-549 (IC50 = 21.0μmol·L-1) and inhibitory activity against cisplatin (IC50 = 19.4μmol·L-1) .The preliminary structure-activity relationship shows that the three-dimensional structure of the compound may have a greater impact on its antitumor activity.