【摘要】 合成一系列黄酮水杨酸衍生物并研究其体外抗肿瘤活性。通过Friedel-Crafts反应和改进后的Baker-Venkataraman重排反应得到化合物2。水杨酸衍生物甲基化和酰氯化后,与化合物2和白杨素发生酯化反应得到目标化合物。采用MTT法检测化合物的体外抗肿瘤活性。化合物2、5a、5b、6a、6b对胃癌细胞MGC-803整体的抗增殖活性更好,均优于白杨素与5-氟尿嘧啶。其中5b对胃癌细胞MGC-803的抗肿瘤活性(21.59±5.75μmol/L)优于其它化合物。黄酮骨架引入苯三甲氧基基团在一定程度上能增强其抗肿瘤活性。化合物5b具有较好的抗肿瘤活性,可作为抗癌候选药物进一步优化和评价。更多还原

【Abstract】 A series of flavonoids salicylate derivatives were synthesised and evaluated for their anti-tumor activity.Compound 2 was synthesised by a Friedel-Crafts reaction and an improved Baker-Venkatarama rearrangement reaction. The anti-tumor activity of compounds was studied by MTT colorimetric assay. On the whole,compounds 2,5 a,5 b,6 a and 6 b showed better anti-tumor activity in MGC-803 cells than chrysin and the positive control 5-Fu. What’s more,Compound 5 b exhibited the most potent anti-proliferative activity against MGC-803 cells with IC50 values of 21. 59 ± 5. 75 μmol/L. The benzene trimethoxy brought certain influence to bioactivity of flavonoids salicylate derivatives. Compound 5 b could be a potential anti-tumor agent after further optimisation and evaluation.更多还原