谭鸿舟,许嘉琛,付俐,刘成波,何黎琴.化学通报,2024,87(2):242-247.
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
投稿时间:2023-07-18  修订日期:2023-08-25
DOI:
中文关键词:  查尔酮  曼尼希碱  丹皮酚  抗癌活性
英文关键词:chalcone  Mannich base  paeonol  anticancer activity
基金项目:安徽省教育厅自然科学科研项目(KJ2020A0957, KJ2021B003)资助
作者单位E-mail
谭鸿舟 安徽中医药大学药学院 337152170@qq.com 
许嘉琛 安徽中医药大学药学院  
付俐 安徽省食品药品检验研究院  
刘成波 安徽中医药大学药学院  
何黎琴* 安徽中医药大学药学院 hlq661125@126.com 
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中文摘要:
      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(HR-MS)、核磁共振氢谱(1H-NMR)、核磁共振碳谱(13C-NMR)进行确证。采用MTT法测试了上述化合物对人肺癌细胞A549、人肝癌细胞HepG2的体外抗增殖活性。实验结果表明,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(5-FU)。
英文摘要:
      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 confirmed by HRMS, 1H NMR and 13C NMR. The in vitro antiproliferative activities of the synthesized compounds were assessed against human cancer cell lines (HepG2 and A549). All of them exhibited good cell proliferation inhibition in HepG2 and A549 cell lines and their antiproliferative activity was significantly better than that of the positive control drug 5-fluorouracil (5-FU) according to the MTT assay.
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