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目的设计并合成新型查尔酮类化合物,初步评价其体外抗肿瘤活性。方法以2,4-二羟基苯乙酮为原料,经酚羟基烷基化、氯甲基化、氮烷基化、羟醛缩合4步反应合成目标化合物。以A-549(人肺腺癌细胞株)、SGC-7901(人胃癌细胞株)、SW-1990(人胰腺癌细胞株)、MCF-7(人乳腺癌细胞株)4种肿瘤细胞为测试细胞株,采用MTT法测定目标化合物的抗肿瘤活性。结果与结论合成了16个新型查尔酮类化合物,其结构经1H-NMR谱确证。体外抗肿瘤活性数据表明:合成的目标化合物具有较好的抗肿瘤活性,可进行更深入的研究。
Objective To design and synthesize new chalcone compounds and evaluate their anti-tumor activity in vitro. Methods 2,4-Dihydroxyacetophenone was used as the starting material to synthesize the target compound by 4-step reaction of phenol hydroxy alkylation, chloromethylation, nitrogen alkylation and aldol condensation. Four tumor cells, A-549 (human lung adenocarcinoma cell line), SGC-7901 (human gastric cancer cell line), SW-1990 (human pancreatic cancer cell line) and MCF-7 (human breast cancer cell line) Cell lines, the anti-tumor activity of the target compounds was determined by MTT assay. RESULTS AND CONCLUSIONS Sixteen novel chalcones were synthesized and their structures were confirmed by 1H-NMR. In vitro antitumor activity data show that: the synthesis of the target compound has good antitumor activity, can be more in-depth study.