查尔酮曼尼希碱类衍生物的设计、合成及抗肿瘤活性研究

Syntheses and Anticancer Activities of Chalcone Mannich Base Derivatives

以丹皮酚和对氯苯甲醛为起始原料,通过Claisen-Schmidt反应得到2-羟基-4-甲氧基-4′-氯查尔酮(3),再经过Mannich反应得到10个查尔酮曼尼希碱衍生物(4a~4e, 5a~5e)。目标化合物结构均经高分辨质谱、核磁共振氢谱、碳谱进行确证。采用MTT法测试了所合成化合物对人肺癌细胞A549、人肝癌细胞HepG2的体外抗增殖活性。结果表明,目标化合物对肿瘤细胞A549、HepG2均具有较强的细胞增值抑制作用,且明显优于阳性对照药5-氟尿嘧啶。

Starting from paeonol and p-chlorobenzaldehyde,the target compounds paeonol mannich base derivatives(4a~4e,5a~5e)were obtained through Claisen-Schmidt and Mannich reactions.The chemical structure of target compounds was confrmed by HRMS,'H NMR and°C NMR.The in vitro antiproliferative activities of the synthesized compounds were assessed against human cancer cell lines(HepG2 and A549).The results showed that the target compounds had strong cell proliferation inhibitory effects on tumor cells A549 and HepG2,and were significantly superior to the positive control drug 5-fluorouracil.