目的：設計2-羥基查耳酮類衍生物的合成路線，并對其進行體外抗腫瘤活性實驗。方法：以2,4-二羥基苯乙酮為原料，經(jīng)過4步反應得到13個5-哌啶基甲基-4-乙氧基-2-羥基-查耳酮類化合物。用MTT法檢測13個目標化合物對對數(shù)生長期的人胃癌細胞株SGC-7901、人結(jié)腸癌細胞株SW-480，人白血病細胞株L1210、人乳腺癌細胞株MCF-7等4種癌細胞株增殖的抑制作用，以研究目標化合物體外抗腫瘤活性。結(jié)果 合成了13個化合物，結(jié)構(gòu)均經(jīng)過H-NMR確證。體外抗腫瘤活性篩選表明，這一類化合物具有良好的抗腫瘤活性。結(jié)論 該合成路線反應溫和、操作簡便、對環(huán)境友好，目標化合物有較強抗腫瘤活性，可進行深入研究。

Objective To design a synthetic route for 2,4-dihydroxychalcone derivatives, and to evaluate their in vitro anti-tumor activities. Methods The substance 2,4-dihydroxyacetophenone was used as staring material. After a series of reactions in four steps, 5-piperidyl-4-ethoxy-2-hydroxy-hydroxy-chalcone derivatives were obained.MTT assay was conducted to detect the prohibitive effects of the target compounds on cancer cell lines, including human gastric carcinoma cell line SGC-7901,colon cancer cell line SW-480,lymphocytic leukemia cell line L1210,and human breast cancer cell line MCF-7.Results Thirteen new compounds were prepared and their structures were confirmed by H-NMR. The in vitro screening showed that these compounds displayed promising anti-tumor activities. Conclusion The synthetic route is easy to operate. The chemical reactions are mild and environmentally friendly. The prepared compounds display promising anti-tumor activities and are worh further studying.