新型查尔酮类化合物的合成及其抗肿瘤活性

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。

Studies on the synthesis and antitumor activity of new series of chalcone derivatives

Aim To design and synthesize a new series of chalcone derivatives and evaluate their antitumor activities. Methods The target compounds were synthesized from 2,4-dihydroxyacetophenone via phenol alkylation, Blanc reaction, N-alkylation and condensation with benzaldehydes, and their in vitro antitumor activity were tested with A-549(human lung adenocarcinoma cell line), SGC-7901(human gastric carcinoma cell line), SW-1990(human pancreatic cancer cell line), MCF-7(human breast cancer cell line). Results and conclusion Sixteen new compounds were prepared and their structures were confirmed by ¹H-NMR. These compounds display promising antitumor activity in vitro and it is worth to be studied in the further.