Synthesis and biological evaluation of novel asymmetric naphthalene diimide derivatives as anticancer agents depending on ROS generation.
Synthesis and biological evaluation of novel asymmetric naphthalene diimide derivatives as anticancer agents depending on ROS generation.
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基于ROS生成的新型不对称萘二酰亚胺衍生物作为抗癌剂的合成和生物学评价。
DOI：
10.1039/c8md00265g
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发表时间：
2018-07
期刊：
影响因子：
--
通讯作者：
Luo Wen
中科院分区：
文献类型：
--
作者：
Xu Xiaojuan;Wang Senzhen;Chang Yuan;Ge Chaochao;Li Xinna;Feng Yongli;Xie Songqiang;Wang Chaojie;Dai Fujun;Luo Wen
萘四甲酸二酰亚胺（NDI）作为光电材料在医药领域有着广泛的应用。合成了一系列不对称萘二酰亚胺衍生物，并通过多种实验方法对其抗癌活性进行了评价。作为代表性化合物，3c对肝癌细胞SMMC-7721和Hep G2的抑制作用显著大于正常肝细胞QSG-7701，其IC 50值分别为1.48 ± 0.43 μM和1.70 ± 0.53 μM，IC 50值为7.11 ± 0.08 μM。化合物3c（3 μM）处理SMMC-7721和Hep G2细胞48 h后，细胞凋亡率分别为52.1%和67.8%。化合物3c以浓度依赖性方式诱导自噬并抑制肝癌细胞的迁移，这是由于活性氧（ROS）的产生。基于其生物活性，化合物3c被认为是有效的抗癌剂。
Naphthalenetetracarboxylic diimide (NDI) is widely used as a photoelectric material in the field of medicine. A series of asymmetric naphthalene diimide derivatives were synthesized and evaluated for their anticancer properties by various experimental assays. As the representative compound, 3c exerted significantly greater inhibitory effects on hepatoma cells SMMC-7721 and Hep G2 with an IC50 value of 1.48 ± 0.43 μM and 1.70 ± 0.53 μM, respectively, than normal hepatocytes QSG-7701 with an IC50 value of 7.11 ± 0.08 μM. Treatment with compound 3c (3 μM) for 48 h resulted in apoptosis of SMMC-7721 cells and Hep G2 cells with 52.1% and 67.8% apoptotic cells, respectively. Compound 3c induced autophagy and suppressed the migration of hepatoma cells in a concentration-dependent manner, resulting from the generation of reactive oxygen species (ROS). Based on its biological ability, compound 3c was considered as a potent anticancer agent.
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影响因子：
64.5
作者：
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通讯作者：
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影响因子：
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通讯作者：
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影响因子：
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作者：
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