期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 181, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.07.023
关键词
Hybrid; 1,2,3-Triazole; Nucleobase; Anti-cancer activity; Migration; Invasion
资金
- Key Scientific and Technological Project of Henan Province [182102310121]
- National Natural Science Foundation of China [81430085]
A series of novel triazole nucleobase analogues containing steroidal/coumarin/quinoline moieties have been synthesized based on copper-catalyzed azide-alkyne cycloaddition (CuAAC). The anti-cancer activity of the new triazole nucleobase analogues was studied in gastric cancer cell lines (MGC-803, SGC-7901) and normal gastric epithelial cells (GES-1) in vitro. Some of the synthesized compounds could significantly inhibit the proliferation of these tested cancer cells. Among the tested compounds, compound 20c demonstrated good anti-proliferation activity against MGC-803 cells (IC50 = 1.48 mu M) and SGC-7901 (IC50 = 2.28 mu M) cells as well as the best selectivity between the cancer and normal cells. Further mechanistic studies indicated that compound 20c could down-regulate the expression of TGF beta 1 both in the tested gastric cancer cell lines and inhibit the cell migration and invasion. The results of the study indicate that compound 20c could be used as a promising skeleton for anti-gastric cancer agents with improved efficacy and less side effects. (C) 2019 Published by Elsevier Masson SAS.
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