期刊
BIOORGANIC CHEMISTRY
卷 107, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2021.104634
关键词
Indole; Apoptosis; NEDDylation pathway; MAPK pathway; MGC803 cells
资金
- National Natural Sciences Foundations of China [81703541, U2004123, 81673322]
- China Postdoctoral Science Foundation [2020M670239, 2018M632812]
- Henan Association of Science and Technology [2020HYTP056]
- Science and Technology Department of Henan Province [20202310144]
- open fund of state key laboratory of Pharmaceutical Biotechnology, Nan-jing University, China [KFGN-202104]
The novel indole derivative V7 showed potent inhibitory activity against MGC803 cancer cells by inhibiting colony formation, inducing apoptosis, and arresting cell cycle at G2/M phase. Moreover, V7 also inhibited the NEDDy-lation pathway and MAPK pathway against MGC803 cells.
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.
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