4-二甲氨基黄酮衍生物的合成及其活性评价有机化学.pdfVIP

DOI: 10.6023/cjoc201309034 研究简报 有机化学 Chinese Journal of Organic Chemistry NOTE 4-二甲氨基黄酮衍生物的合成及其活性评价 苏亚彬 洪 琛 李 骞 罗 稳* 王超杰* (河南大学 天然药物与免疫工程重点实验室 开封 475004) 摘要 设计合成了 10 个 4-二甲氨基黄酮衍生物, 产物结构均经 1H NMR, ESI-MS 和元素分析确认. 采用噻唑蓝(MTT) 法测试了化合物对 HepG2(人肝癌细胞) 的抑制作用, 结果表明目标化合物在 30 μmol/L 浓度下对 HepG2 细胞损伤均有 一定的抑制作用, 大部分化合物优于对照药物槲皮素, 其中化合物 5c, 5e, 5f 和 5j 活性最强, 抑制率分别为 91.0%, 90.1%, 95.7%和 92.1%, 而且化合物 5f 在 10 μmol/L 浓度下对 HepG2 的抑制率为93.1%, 具有深入研究的价值. 关键词 黄酮; 衍生物; 合成; 抗肿瘤 Synthesis and Biological Evaluation of 4-Dimethylamino Flavonoid Derivatives Su, Yabin Hong, Chen Li, Qian Luo, Wen* Wang, Chaojie* (Key Laboratory of Natural Medicine and Immuno-Engineering of Henan Province, Henan University, Kaifeng 475004) Abstract Ten novel 4-dimethylamino flavonoid derivatives were designed and synthesized. The structures of these com- pounds were confirmed by 1H NMR, ESI-MS and elemental analysis. Their preliminary antitumor activity was evaluated by measuring their cytotoxic activity against the HepG2 cell line using thiazolyl blue tetrazolium bromide (MTT) assay. All ten compounds exhibited potent antitumor activity at 30 μmol/L. Some of the compounds displayed higher activity than the refer- ence compound, quercetin. Compounds 5c, 5e, 5f and 5j were the most potent with inhibition rates of 91.0%, 90.1%, 95.7% and 92.1%, respectively. Moreover, compound 5f at 10 μmol/L showed an inhibition rate of 93.1%. Further investigation is needed. Keywords flavonoid; derivative; synthesis; antitumor 黄酮(Fl