Discovery of novel indole derivatives that inhibit NEDDylation and MAPK pathways against gastric cancer MGC803 cells
Discovery of novel indole derivatives that inhibit NEDDylation and MAPK pathways against gastric cancer MGC803 cells
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发现新型吲哚衍生物，可抑制胃癌 MGC803 细胞的 NEDDylation 和 MAPK 途径。
DOI：
10.1016/j.bioorg.2021.104634
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发表时间：
2021-01-18
影响因子：
5.1
通讯作者：
Zhang, Sai-Yang
中科院分区：
文献类型：
--
作者：
Fu, Dong-Jun;Cui, Xin-Xin;Zhang, Sai-Yang
合成了一系列新型吲哚衍生物，并评价了它们对三种选定的癌细胞系（MGC 803，EC-109和PC-3）的抗增殖活性。在这些类似物中，2-（5-甲氧基-1H-吲哚-1-基）-N-（4-甲氧基苄基）-N-（3，4，5-三甲氧基苯基乙酰胺（V7）对MGC 803细胞的抑制活性最好，IC 50值为1.59 μ M。细胞机制阐明了V7抑制集落形成、诱导细胞凋亡、使细胞周期阻滞于G2/M期。重要的是，吲哚类似物V7抑制NEDDy-化途径和MAPK途径对MGC 803细胞的杀伤作用。
A series of novel indole derivatives were synthesized and evaluated for their antiproliferative activity against three selected cancer cell lines (MGC803, EC-109 and PC-3). Among these analogues, 2-(5-methoxy-1H-indol-1-yl)-N-(4-methoxybenzyl)-N-(3,4,5-trimethoxyphenyeacetamide (V7) showed the best inhibitory activity against MGC803 cells with an IC50 value of 1.59 mu M. Cellular mechanisms elucidated that V7 inhibited colony formation, induced apoptosis and arrested cell cycle at G2/M phase. Importantly, indole analogue V7 inhibited NEDDy-lation pathway and MAPK pathway against MGC803 cells.