摘要/Abstract
主要通过Claisen-Schmidt缩合反应设计合成了一系列含有哌啶、吗啡啉、N-甲基哌嗪取代的查尔酮衍生物，并通过噻唑蓝（MTT）法对MCF-7（人乳腺癌细胞系）、A549（人肺癌细胞系）、HL-60（人白血病细胞系）、Hela（人宫颈癌细胞系）和Bewo（人绒毛肿瘤细胞系）等五种癌细胞系进行了体外抗癌活性研究.研究表明，化合物4a，4e，4f，4j，4m，4o对MCF-7，A549，HL-60三种癌细胞系抗癌活性最佳，IC50值均在10 μmol/L以下.
关键词: 查尔酮, 缩合, 抗癌, MTT法
Three series of chalcones bearing a piperidino, morpholino, and 1-methylpiperazino moiety were synthesized in two steps with the key step being Claisen-Schmidt condensation and tested for the activity against five cell lines, MCF-7 (human breast adenocarcinoma cell line), A549 (human lung adenocarcinoma epithelial cell line), HL-60 (human leukemia cell line), Hela (human cervical cancer cell line), and Bewo (human chorionic tumor cell line) by thiazolyl blue tetrazolium bromide (MTT) assay. Some chalcones exhibited good anticancer activity, and among them 4a, 4e, 4f, 4j, 4m, and 4o displayed the best anticancer activity for MCF-7 breast cancer cells, A549 lung cancer cells, and HL-60 leukemia cancer cells with IC50 values below 10 μmol/L, respectively.
Key words: chalcone, condensation, anticancer agents, MTT assay
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