Flavone inspired discovery of benzylidenebenzofuran-3(2H)-ones (aurones) as potent inhibitors of human protein kinase CK2

[Display omitted] •New substituted benzylidenebenzofuran-3(2H)-ones were synthesized.•41 aurones inhibited CK2 with IC50 in nanomolar range of values.•The most promising compound 12m (BFO13) has an IC50 = 3.6 nM with CLipE = 4.94. In this work, we describe the design, synthesis and SAR studies of 2-...

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Veröffentlicht in:	Bioorganic chemistry 2020-09, Vol.102, p.104062-104062, Article 104062
Hauptverfasser:	Protopopov, M.V., Vdovin, V.S., Starosyla, S.A., Borysenko, I.P., Prykhod'ko, A.O., Lukashov, S.S., Bilokin, Y.V., Bdzhola, V.G., Yarmoluk, S.M.
Format:	Artikel
Sprache:	eng
Schlagworte:	2-benzylidenebenzofuran-3-ones Aurone Benzofurans - pharmacology Benzofurans - therapeutic use Casein Kinase II - chemistry Flavones - pharmacology Flavones - therapeutic use Humans In vitro biochemical assay Molecular docking Molecular Docking Simulation - methods Protein kinase CK2 inhibitor Structure-Activity Relationship Virtual screening
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