摘要
通过2-甲基-4-氧代喹唑啉-6-甲醛与不同的吲哚-2-酮的缩合反应,制备了一系列吲哚-2-酮与喹唑啉-4(3H)-酮的杂合物5a–j。MTT法测试结果表明,只有化合物5e对人肿瘤细胞A549、MCF-7、He La、HT-29和HCT-116表现出一定的细胞毒活性,50μM浓度下的抑制率为32.0%–62.3%。
A novel series of compounds combining indolin-2-one and quinazolin-4（3H）-one moiety via a carbon-carbon double bond were synthesized by aldol-condensation of 2-methylquinazolin-4（3H）-one-6-carbaldehyde with various indolin-2-ones. The synthesized compounds were evaluated for their cytotoxic activity against five human cancer cell lines, namely, A549, MCF-7, HeLa, HT-29 and HCT-116. We found that compound 5e with two bromine atoms at the 5- and 7-positions of the indolin-2-one ring was most potent, which inhibited proliferation of five cancer cell lines in the range of 32.0%-62.3% at a concentration of 50 p,M. Our results further indicate that the connection of 5,7-dibromoindolin-2-one and 2-methylquinazolin- 4（3H）-one moiety with a carbon-carbon double bond is essential for compound 5e to exert cytotoxicity.
基金
National Natural Science Foundation of China (Grant No.20972099,31130017)
Beijing Municipal Commission of Education (Grant No.KZ201210028035)
Scientific Research Base Development Program of the Beijing Municipal Commission of Education
the 973 Project (Grant No.2013CB911000)
