Potential anticancer agents. I. Synthesis of isoxazole moiety containing quinazoline derivatives and preliminarily in vitro anticancer activity.

Potential anticancer agents. I. Synthesis of isoxazole moiety containing quinazoline derivatives and preliminarily in vitro anticancer activity.
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DOI:
10.2174/1871520614666140812105445
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发表时间:
2014-12
影响因子:
2.8
通讯作者:
Jianping Yong;Canzhong Lu;Xiaoyuan Wu
Jianping Yong;Canzhong Lu;Xiaoyuan Wu
中科院分区:
医学4区
文献类型:
--
作者:
Jianping Yong;Canzhong Lu;Xiaoyuan Wu

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首次合成了14个新结构的含异恶唑基喹唑啉衍生物(3a~3n),并通过IR、(1)H NMR、(13)C NMR、ESI-MS进行了表征。随后,采用MTT法初步评价了它们对A549、HCT116和MCF-7细胞系的体外抗癌活性。其中,大多数化合物表现出良好至优异的抗癌活性,尤其是3d、3i、3k和3m对A549、HCT116和MCF-7细胞系表现出更强的抗癌活性,可被视为抗癌药物开发的有希望的候选药物。
14 new structures of isoxazole-moiety-containing quinazoline derivatives(3a~3n) were synthesized for the first time and characterized by IR, (1)H NMR, (13)C NMR, ESI-MS. Subsequently, their in vitro anticancer activity against A549, HCT116 and MCF-7 cell lines was preliminarily evaluated using the MTT method. Among them, most compounds showed good to excellent anticancer activity, especially 3d, 3i, 3k and 3m exhibited the more potent anticancer activity against A549, HCT116 and MCF-7 cell lines, which can be regarded as the promising drug candidates for development of anticancer drugs.