Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases

[Display omitted] The tankyrases are members of the PARP superfamily; they poly(ADP-ribosyl)ate their target proteins using NAD+ as a source of electrophilic ADP-ribosyl units. The three principal protein substrates of the tankyrases (TRF1, NuMA and axin) are involved in replication of cancer cells;...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2015-07, Vol.23 (13), p.3013-3032
Hauptverfasser:	Kumpan, Katerina, Nathubhai, Amit, Zhang, Chenlu, Wood, Pauline J., Lloyd, Matthew D., Thompson, Andrew S., Haikarainen, Teemu, Lehtiö, Lari, Threadgill, Michael D.
Format:	Artikel
Sprache:	eng
Schlagworte:	7-Aryl-1-methyl-1,2,3,4-tetrahydro-1,6-naphthyridin-5-one Ammonia - chemistry Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Aza Compounds - chemistry Benzamidines - chemistry Carboxylic Acids - chemistry Crystal structure Crystallography, X-Ray Cyclization Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Heterocyclic Compounds, 3-Ring - chemistry Humans Ketones - chemistry Molecular Docking Simulation Naphthyridines - chemical synthesis Naphthyridines - chemistry Naphthyridinone Nitriles - chemistry Pyrimidinones - chemical synthesis Pyrimidinones - chemistry Structure-Activity Relationship Tankyrase Tankyrases - antagonists & inhibitors Tankyrases - chemistry TNKS
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