发现新型吲哚衍生物，抑制 NEDDylation 和 MAPK 通路，用于治疗胃癌 MGC803 细胞。
Discovery of novel indole derivatives that inhibit NEDDylation and MAPK pathways against gastric cancer MGC803 cells.
机构信息
Modern Research Center for Traditional Chinese Medicine, School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100029, China.
School of Basic Medical Science, Zhengzhou University, Zhengzhou 450001, China.
出版信息
Bioorg Chem. 2021 Feb;107:104634. doi: 10.1016/j.bioorg.2021.104634. Epub 2021 Jan 8.
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-trimethoxyphenyl)acetamide (V7) showed the best inhibitory activity against MGC803 cells with an IC value of 1.59 μM. Cellular mechanisms elucidated that V7 inhibited colony formation, induced apoptosis and arrested cell cycle at G2/M phase. Importantly, indole analogue V7 inhibited NEDDylation pathway and MAPK pathway against MGC803 cells.
一系列新型吲哚衍生物被合成并评估了它们对三种选定的癌细胞系（MGC803、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 MGC803 细胞表现出最好的抑制活性，IC 值为 1.59 μM。细胞机制阐明，V7 抑制集落形成，诱导细胞凋亡并将细胞周期阻滞在 G2/M 期。重要的是，吲哚类似物 V7 抑制了 NEDDylation 途径和 MAPK 途径对 MGC803 细胞的作用。
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