2-羟基查耳酮类衍生物的合成与抗肿瘤活性筛选  

Synthesis of 2-hydroxychalcone derivatives and anti-tumor activity screening

作　　者：石玉[1] 李祎亮[1] 刘巍[1] 邹美香[1] 赵乐晶[2] 

机构地区：[1]天津药物研究院天津市新药设计与发现重点实验室,天津300193 [2]沈阳药科大学,辽宁沈阳110016

出　　处：《现代药物与临床》2010年第1期48-52,共5页Drugs & Clinic

摘　　要：目的设计2-羟基查耳酮类衍生物的合成路线,并对其进行体外抗肿瘤活性实验。方法以2,4-二羟基苯乙酮为原料,经过4步反应得到13个5-哌啶基甲基-4-乙氧基-2-羟基-查耳酮类化合物。用MTT法检测13个目标化合物对对数生长期的人胃癌细胞株SGC-7901、人结肠癌细胞株SW-480、人白血病细胞株L1210、人乳腺癌细胞株MCF-7等4种癌细胞株增殖的抑制作用,以研究目标化合物体外抗肿瘤活性。结果合成了13个目标化合物,结构均经过1H-NMR确证。体外抗肿瘤活性筛选表明,这一类化合物具有良好的抗肿瘤活性。结论该合成路线反应温和、操作简便、对环境友好,目标化合物有较强抗肿瘤活性,可进行深入研究。Objective To design a synthetic route for 2, 4-dihydroxy-chalcone derivatives, and to evaluate their in vitro anti-tumor activities. Methods The substance 2, 4-dihydroxyacetophenone was used as starting material. After a series of reactions in four steps, 5-piperidyl-4-ethoxy-2-hydroxy-chalcone derivatives were obtained. 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 ell line MCF-7. Results Thirteen new compounds were prepared and their structures were confirmed by ^1H-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 worth further studying.

关 键 词：2-羟基查耳酮衍生物 化学合成 药理作用 抗肿瘤 

分 类 号：R914.5[医药卫生—药物化学] R979.19[医药卫生—药学]