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

作　　者：谭鸿舟 许嘉琛 付俐 刘成波 何黎琴 Tan Hongzhou;Xu Jiachen;Fu Li;Liu Chengbo;He Liqin(College of Pharmacy,Anhui University of Chinese Medicine,Hefei,23001l;Anhui Institute for Food and Drug Control,Hefei,230051)

机构地区：[1]安徽中医药大学药学院,合肥230011 [2]安徽省食品药品检验研究院,合肥230051

出　　处：《化学通报》2024年第2期242-247,共6页Chemistry

基　　金：安徽省教育厅自然科学科研项目(KJ2020A0957,KJ2021B003)资助。

摘　　要：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.

关 键 词：查尔酮 曼尼希碱 丹皮酚 抗癌活性 

分 类 号：TQ463[化学工程—制药化工]