New application of novel tetrazine derivatives as potent VEGFR-2 kinase inhibitors and anti-cancer agents
Background: A novel series of s-tetrazine derivatives was designed as a new scaffold and synthesized efficiently as VEGFR-2 inhibitors for the first time. Methodology & results: The inhibitory activities of the new compounds were tested by MTT assay and enzyme assay, respectively. Western blot assay, cell apoptosis assay and cell migration assay were carried out to study the action mechanism of them. All the synthesized compounds showed evident VEGFR-2 inhibitory activities (IC50 in the range of 88.53-257.55 nM). Compounds 23h, 25d, 26e and 27c showed excellent anti-proliferative activities against the four tested cell lines and were better than sorafenib basically. Conclusion: Compounds with good activities based on this novel scaffold can be screened successfully.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:14 |
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| Enthalten in: |
Future medicinal chemistry - 14(2022), 17 vom: 26. Sept., Seite 1251-1266 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Zheng, Quan [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 24.08.2022 Date Revised 06.09.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2022-0054 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM344698335 |
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| 520 | |a Background: A novel series of s-tetrazine derivatives was designed as a new scaffold and synthesized efficiently as VEGFR-2 inhibitors for the first time. Methodology & results: The inhibitory activities of the new compounds were tested by MTT assay and enzyme assay, respectively. Western blot assay, cell apoptosis assay and cell migration assay were carried out to study the action mechanism of them. All the synthesized compounds showed evident VEGFR-2 inhibitory activities (IC50 in the range of 88.53-257.55 nM). Compounds 23h, 25d, 26e and 27c showed excellent anti-proliferative activities against the four tested cell lines and were better than sorafenib basically. Conclusion: Compounds with good activities based on this novel scaffold can be screened successfully | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 4 | |a enzyme inhibitory | |
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| 650 | 4 | |a molecular docking | |
| 650 | 4 | |a s-tetrazine | |
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| 700 | 1 | |a Jin, Hao |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Wen |e verfasserin |4 aut | |
| 700 | 1 | |a Rao, Guo-Wu |e verfasserin |4 aut | |
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