A π-Halogen Bond of Dibenzofuranones with the Gatekeeper Phe113 in Human Protein Kinase CK2 Leads to Potent Tight Binding Inhibitors

A π-Halogen Bond of Dibenzofuranones with the Gatekeeper Phe113 in Human Protein Kinase CK2 Leads to Potent Tight Binding Inhibitors

Human protein kinase CK2 is an emerging target for neoplastic diseases. Potent lead structures for human CK2 inhibitors are derived from dibenzofuranones. Two new derivatives, 7,9-dichloro-1,2-dihydro-8-hydroxy-4-[(4-methoxyphenylamino)-methylene]dibenzo[b,d]furan-3(2H)-one (4a) and (E)-1,3-dichloro...

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Bibliographic Details
Main Authors: Alexander Schnitzler, Andreas Gratz, Andre Bollacke, Michael Weyrich, Uwe Kuckländer, Bernhard Wünsch, Claudia Götz, Karsten Niefind, Joachim Jose
Format: Article
Language:English
Published: MDPI AG 2018-02-01
Series:Pharmaceuticals
Subjects:
human protein kinase CK2
dibenzofuran
tight binding inhibitor
crystal structure
π-halogen bond
apoptosis induction
Online Access:http://www.mdpi.com/1424-8247/11/1/23

Internet

http://www.mdpi.com/1424-8247/11/1/23

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