Synthesis and anti-gastric cancer activity evaluation of novel triazole nucleobase analogues containing steroidal/coumarin/quinoline moieties
| Autor: | Hong-Min Liu, Zhao Jianwei, Zeng-Hui Wu, Ya-Zhen You, Ming-Jie Huang, Li-Hua Huang, Jia-Wen Guo |
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| Rok vydání: | 2019 |
| Předmět: |
1
2 3-Triazole Stereochemistry Triazole Antineoplastic Agents 01 natural sciences Nucleobase 03 medical and health sciences chemistry.chemical_compound Structure-Activity Relationship Coumarins Stomach Neoplasms Drug Discovery medicine Tumor Cells Cultured Humans 030304 developmental biology Cell Proliferation Pharmacology 0303 health sciences Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Organic Chemistry Quinoline Cancer Cell migration General Medicine Triazoles medicine.disease Coumarin 0104 chemical sciences chemistry Cancer cell Quinolines Steroids Drug Screening Assays Antitumor |
| Zdroj: | European journal of medicinal chemistry. 181 |
| ISSN: | 1768-3254 |
| Popis: | 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 μM) and SGC-7901 (IC50 = 2.28 μM) 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 β1 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. |
| Databáze: | OpenAIRE |
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