Synthesis and Biological Evaluation of Quinazoline Derivatives as Potential Anticancer Agents (II).
Synthesis and Biological Evaluation of Quinazoline Derivatives as Potential Anticancer Agents (II).
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DOI：
10.2174/1871520615666150526115904
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发表时间：
2015-11
影响因子：
2.8
通讯作者：
Jianping Yong;Canzhong Lu;Xiaoyuan Wu
中科院分区：
文献类型：
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作者：
Jianping Yong;Canzhong Lu;Xiaoyuan Wu
在前期工作的指导下，我们合成了21个新结构的喹唑啉类化合物（3a~3u），并采用MTT法评价了它们对A549、HCT 116和MCF-7细胞的体外抗癌活性。大多数化合物显示出良好至优异的抗癌活性。特别是，3 o（被认为是厄洛替尼类似物）对A549、HCT 116和MCF-7细胞系具有显著的抗癌活性（IC 50分别为4.26、3.92和0.14 μM），与标准抗癌药物吉非替尼相比（IC 50分别为17.9、21.55和20.68 μM），可视为开发抗癌药物的最佳候选药物。
Under the guidance of our previous work, we synthesized 21 new structures of quinazolines (3a~3u) and evaluated their in vitro anticancer activity against A549, HCT116 and MCF-7 cell lines using the MTT method. Most compounds showed good to excellent anticancer activity. In particular, 3o (regarded as erlotinib analogues) has marked anticancer activity against A549, HCT116 and MCF-7 cell lines (IC50s: 4.26, 3.92 and 0.14 μM, respectively) as compared with the standard anticancer drug gefitinib (IC50s: 17.9, 21.55 and 20.68 μM, respectively), and which can be regarded as the best candidate for development of anticancer drugs.