Discovery of Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia

Bromodomain-selective BET inhibition has emerged as a promising strategy to improve the safety profiles of pan-BET inhibitors. Herein, we report the discovery of potent phenoxyaryl pyridones as highly BD2-selective BET inhibitors. Compound 23 (IC50 = 2.9 nM) exhibited a comparable BRD4 BD2 inhibitor...

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Veröffentlicht in:	Journal of medicinal chemistry 2024-01, Vol.67 (2), p.1513-1532
Hauptverfasser:	Jiang, Wenhua, Hou, Qiangqiang, Xu, Hongrui, Yang, Kexin, Wang, Xiaohui, Zhang, Kuojun, Zeng, Yi, Li, Wenqiang, Wang, Bingrui, Luo, Guangmei, Zhao, Xiaofan, Shen, Hui, Xu, Yong, Wu, Xiaoxing
Format:	Artikel
Sprache:	eng
Online-Zugang:	Volltext
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