Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors

[Display omitted] Bromodomain-containing protein 4 (BRD4) is a key epigenetic regulator in cancer, and inhibitors targeting BRD4 exhibit great anticancer activity. By replacing the methyltriazole ring of the BRD4 inhibitor I-BET-762 with an N-methylthiazolidone heterocyclic ring, fifteen novel BRD4...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2020-08, Vol.28 (15), p.115601-115601, Article 115601
Hauptverfasser:	Li, Qifei, Li, Jieming, Cai, Yan, Zou, Yuxing, Chen, Bin, Zou, Feng, Mo, Jiaxian, Han, Ting, Guo, Weiwei, Huang, Wenlong, Qiu, Qianqian, Qian, Hai
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-proliferation Anti-tumor Apoptosis BRD4 inhibitors
Online-Zugang:	Volltext
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