Novel HIF-1α inhibitor CDMP-TQZ for cancer therapy
Aim: Tumor cells adapt to hypoxic microenvironments by releasing the key transcription factor HIF-1α, which promotes angiogenesis, glycolytic phenotype, metastasis and erythropoiesis, allowing proliferation amid low oxygen levels. Therefore, therapeutic targeting of HIF-1α represents a viable strategy for cancer therapy. Methods & Results: The authors synthesized a series of novel tetrahydroquinazoline derivatives in six steps and demonstrated that their development had a unique ability to suppress HIF-1α expression through proteasomal degradation. Conclusion: Among these compounds, CDMP-TQZ (8bf) exhibited the highest antiproliferative potency in human cancer cells, in part through downregulation of HIF-1α.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:13 |
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| Enthalten in: |
Future medicinal chemistry - 13(2021), 12 vom: 07. Juni, Seite 1057-1072 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Chu, Po-Chen [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 18.10.2021 Date Revised 18.10.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2020-0307 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM324497555 |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: Tumor cells adapt to hypoxic microenvironments by releasing the key transcription factor HIF-1α, which promotes angiogenesis, glycolytic phenotype, metastasis and erythropoiesis, allowing proliferation amid low oxygen levels. Therefore, therapeutic targeting of HIF-1α represents a viable strategy for cancer therapy. Methods & Results: The authors synthesized a series of novel tetrahydroquinazoline derivatives in six steps and demonstrated that their development had a unique ability to suppress HIF-1α expression through proteasomal degradation. Conclusion: Among these compounds, CDMP-TQZ (8bf) exhibited the highest antiproliferative potency in human cancer cells, in part through downregulation of HIF-1α | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a anticancer agents | |
| 650 | 4 | |a hypoxia-inducible factor-1 | |
| 650 | 4 | |a tetrahydroquinolines | |
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| 650 | 7 | |a Hypoxia-Inducible Factor 1, alpha Subunit |2 NLM | |
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| 700 | 1 | |a Chen, Chien-Yu |e verfasserin |4 aut | |
| 700 | 1 | |a Hung, Yu-Syuan |e verfasserin |4 aut | |
| 700 | 1 | |a Chang, Chih-Shiang |e verfasserin |4 aut | |
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