1,4-二脂肪氨基-5,8-二羟基蒽醌的合成及抗癌活性研究

Synthesis,characterization and anticancer activity of 1,4-bialiphatic amino-5,8-dihydroxy anthraquinones

合成抗癌药物中间体脂肪胺取代的蒽醌类化合物,并对其进行体外抗癌活性测试.以1,4,5,8-四羟基蒽醌隐色体和脂肪胺为原料,在氮气保护下进行缩合反应,然后通过氧化合成目标化合物.对目标化合物利用红外光谱和核磁共振氢谱进行表征.体外抗癌活性测试表明化合物1,4-二[2-(二甲氨基)-乙氨基]-5,8-二羟基蒽醌有较强的抗癌活性.

1,4- Bialiphatic amino-5,8-dihydroxy anthraquinones as an intermediate of an anticancer drug were synthesized by the condensation and oxidation of leuco- 1,4,5,8- tetrahydroxyanthraquinone with aliphatic amine. Their structures were determined by FTIR and l H-NMR analysis. Anti-cancer activities of these compounds were roughly tested in vitro. Such 1,4- bi [ 2 （ dimethylamio ） -ethylamino ] - 5,8- dihydroxy-anthraquinone derivates made this a versatile strategy for the lead compound of anti-tumor drug.