Synthesis and Profiling of a Novel Potent Selective Inhibitor of CHK1 Kinase Possessing Unusual N-trifluoromethylpyrazole Pharmacophore Resistant to Metabolic N-dealkylation

Checkpoint-mediated dependency of tumor cells can be deployed to selectively kill them without substantial toxicity to normal cells. Specifically, loss of CHK1, a serine threonine kinase involved in the surveillance of the G -M checkpoint in the presence of replication stress inflicted by DNA-damagi...

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Veröffentlicht in:Molecular cancer therapeutics 2017-09, Vol.16 (9), p.1831-1842
Hauptverfasser: Samadder, Pounami, Suchánková, Tereza, Hylse, Ondřej, Khirsariya, Prashant, Nikulenkov, Fedor, Drápela, Stanislav, Straková, Nicol, Vaňhara, Petr, Vašíčková, Kateřina, Kolářová, Hana, Binó, Lucia, Bittová, Miroslava, Ovesná, Petra, Kollár, Peter, Fedr, Radek, Ešner, Milan, Jaroš, Josef, Hampl, Aleš, Krejčí, Lumír, Paruch, Kamil, Souček, Karel
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Sprache:eng
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