为开发低毒、高效的蒽醌类抗肿瘤化合物,设计并利用N-烷氨基氮杂糖与大黄酸的缩合反应,及N-烷氨基氮杂糖与1-氨基-4-溴蒽酮-2-磺酸的微波促进Cu0催化乌尔曼偶联(Ullmann coupling)反应,合成系列新型氮杂糖修饰的蒽醌衍生物.对所合成的化合物进行了初步体外肿瘤细胞(Hela、A549、MCF-7和MGC-803)的细胞毒性测试.
In order to develop the anti-tumor agents with high efficiency and low toxicity, a series of novel azasugar modified anthraquinone derivatives have been designed and synthesized by the ammonolysis of N-alkylamino azasugar with rhine and microwave assisted Ullmann coupling reaction ofN-alkylamino azasugar with 1-amino-4-bromoanthraquinone-2-sulfonic acid. Their cytotoxic activities against Hela, A549, MCF-7 and MGC-803 cells were preliminarily evaluated.