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以2,4-喹唑啉二酮为起始原料,通过氯代、Suzuki偶联和芳环亲核取代反应得到一系列2-取代苯氨基喹唑啉衍生物,并经~1H NMR,~(13)C NMR和HRMS进行结构确证.应用溴化噻唑蓝四氮唑(MTT)法对目标化合物进行了初步体外抗肿瘤细胞增殖活性研究.结果表明,部分化合物具有较好的体外抗肿瘤细胞增殖活性,其中活性化合物4u和4v对Hela,A549和MCF-7三种肿瘤细胞株的增殖均有明显抑制作用.
A series of 2-substituted anilinoquinazoline derivatives were obtained from 2,4-quinazolinediones by chlorination, Suzuki coupling and aromatic ring nucleophilic substitution reaction. Their structures were confirmed by ~ 1H NMR, (13) C NMR and HRMS were used to confirm the structure of the target compound.METHODS The target compound was preliminarily studied in vitro by MTT method.The results showed that some of the compounds had good antitumor activity in vitro Proliferative activity, the active compounds 4u and 4v on Hela, A549 and MCF-7 three tumor cell lines were significantly inhibited proliferation.