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以香叶木素或野漆树苷为原料,经过O-甲基化、酸性水解、O-苄基化和过氧丙酮(DMDO)氧化等反应步骤,合成了5,7,3’,4’-四甲氧基黄酮醇(1),5,7,3’-三苄氧基-4’-甲氧基黄酮醇(2),5,7,4’-三甲氧基黄酮醇(3),金合欢素(4)和5,7-二羟基-4’-苄氧基黄酮(5),运用“点击化学”方法,将所合成黄酮类的炔基化合物6～10与β-叠氮化乙酰基半乳糖通过铜催化的1,3-偶极环加成反应链接起来,合成了一系列未见文献报道的新型黄酮半乳糖缀合物11～20.MTT蛋白染色法体外抗肿瘤细胞生物活性测试发现,化合物11,13和20对白血病细胞(HL-60)、肝癌细胞(SMMC-7721)、乳腺癌细胞(MCF-7)、结肠癌细胞(SW480)和肺癌细胞(A-549)具有一定的抑制活性.
In this paper, 5,7,3 ’, 4’- (5’, 5 ’, 5’, 6’- Tetramethoxyflavone alcohol (1), 5,7,3’-tribenzyloxy-4’-methoxyflavone alcohol (2), 5,7,4’-trimethoxyflavone alcohol (3), (4) and 5,7-dihydroxy-4’-benzyloxyflavone (5) using the “click chemistry” method, the synthesized flavonoids alkynyl compounds 6 to 10 and β-stack A series of novel flavonoid galactose conjugates 11 ~ 20 were synthesized by copper-catalyzed 1,3-dipolar cycloaddition reaction of acetylated acetylgalactosamine with 11 ~ 20. MTT protein staining in vitro anti-tumor The cytotoxic activity of compounds 11, 13 and 20 on leukemia cells (HL-60), liver cancer cells (SMMC-7721), breast cancer cells (MCF-7), colon cancer cells (SW480) and lung cancer cells (A- 549) has a certain inhibitory activity.