Novel HIF-1α inhibitor CDMP-TQZ for cancer therapy
In: Future Medicinal Chemistry, Jg. 13 (2021-06-01), S. 1057-1072
Online
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Zugriff:
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.
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Novel HIF-1α inhibitor CDMP-TQZ for cancer therapy
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Autor/in / Beteiligte Person: | Chu, Po-Chen ; Hung, Yu-Syuan ; Chen, Chien-Yu ; Chang, Chih-Shiang ; Wu, Yu-Chieh |
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Zeitschrift: | Future Medicinal Chemistry, Jg. 13 (2021-06-01), S. 1057-1072 |
Veröffentlichung: | Future Science Ltd, 2021 |
Medientyp: | unknown |
ISSN: | 1756-8927 (print) ; 1756-8919 (print) |
DOI: | 10.4155/fmc-2020-0307 |
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