新型查尔酮衍生物的合成及抗肿瘤活性评价
Synthesis and Evaluation of Chalcone Derivatives as Novel Anticancer Agents
Received date: 2018-08-29
Revised date: 2018-10-23
Online published: 2018-11-26
盛琦威 , 赵婉秋 , 曾明 , 谢中袍 , 夏雅平 , 崔冬梅 . 新型查尔酮衍生物的合成及抗肿瘤活性评价[J]. 有机化学, 2019 , 39(3) : 703 -708 . DOI: 10.6023/cjoc201808037
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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