新型 4-氨基喹唑啉衍生物的合成及量子化学研究：作为 Aurora A/B 激酶抑制剂。
Synthesis and quantum chemical studies of new 4-aminoquinazoline derivatives as Aurora A/B kinase inhibitors.
机构信息
School of Biological Science & Medical Engineering, Southeast University, Nanjing 211189, China.
出版信息
Chem Biol Drug Des. 2013 Mar;81(3):399-407. doi: 10.1111/cbdd.12089. Epub 2012 Dec 26.
Nine novel 4-aminoquinazoline derivatives were designed and synthesized. Biochemical and cellular analyses demonstrated that most of the derivatives exhibited a strong activity to inhibit Aurora A and B kinases and to suppress the proliferation of a panel of human tumor cell lines (U937, K562, A549, LoVo, and HT29). Quantum chemical studies were also carried out to determine the structural features of these compounds engaged in the inhibition of Aurora kinases.
设计并合成了 9 种新型 4-氨基喹唑啉衍生物。生化和细胞分析表明，大多数衍生物对抑制 Aurora A 和 B 激酶以及抑制一系列人肿瘤细胞系（U937、K562、A549、LoVo 和 HT29）的增殖具有很强的活性。还进行了量子化学研究，以确定这些化合物抑制 Aurora 激酶的结构特征。
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