Discovery of novel coumarin derivatives as potent and orally bioavailable BRD4 inhibitors based on scaffold hopping

The bromodomain and extra-terminal (BET) bromodomains, particularly BRD4, have been identified as promising therapeutic targets in the treatment of many human disorders such as cancer, inflammation, obesity, and cardiovascular disease. Recently, the discovery of novel BRD4 inhibitors has garnered su...

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Veröffentlicht in:Journal of enzyme inhibition and medicinal chemistry 2019-01, Vol.34 (1), p.808-817
Hauptverfasser: Zhang, Zhimin, Gu, Lili, Wang, Beibei, Huang, Wenhai, Zhang, Yanmin, Ma, Zhen, Zeng, Shenxin, Shen, Zhengrong
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Sprache:eng
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