Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives
Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives
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4-苯胺喹啉衍生物的合成及其抗肿瘤活性
DOI：
10.3390/molecules21010021
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发表时间：
2016-01-01
期刊：
影响因子：
4.6
通讯作者：
Wang, Hai-Feng
中科院分区：
文献类型：
--
作者：
Liu, Dan;Luan, Tian;Wang, Hai-Feng
设计并合成了22个7-氟（或8-甲氧基）-4-苯胺基喹啉类化合物，它们具有潜在的抗肿瘤活性和选择性。所有制备的化合物进行了评价，其在体外抗增殖活性对HeLa和BGC 823细胞系。10个化合物（1a-g; 2c; 2 e和2 i）显示出良好的抗肿瘤活性，其活性上级优于吉非替尼。在这10个化合物中，有7个化合物（1a-c; 1 e-1g和2 i）对BGC 823细胞显示出良好的选择性。特别是，1f和2 i对HeLa细胞和BGC 823细胞表现出较强的细胞毒活性，IC 50值优于吉非替尼。
Twenty-two 7-fluoro (or 8-methoxy)-4-anilinoquinolines compounds were designed and synthesized as potentially potent and selective antitumor inhibitors. All the prepared compounds were evaluated for their in vitro antiproliferative activities against the HeLa and BGC823 cell lines. Ten compounds (1a-g; 2c; 2e and 2i) exhibited excellent antitumor activity superior to that of gefitinib. Among the ten compounds; seven (1a-c; 1e-1g and 2i) displayed excellent selectivity for BGC823 cells. In particular; 1f and 2i exhibited potent cytotoxic activities against HeLa cells and BGC823 cells with better IC50 values than gefitinib.