4-Arylazo-3, 5-diamino-1 H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects

…, M Hajdúch, J Srovnal, WF de Azevedo…

文献索引：Krystof, Vladimir; Cankar, Petr; Frysova, Iveta; Slouka, Jan; Kontopidis, George; Dzubak, Petr; Hajduch, Marian; Srovnal, Josef; De Azevedo Jr., Walter F.; Orsag, Martin; Paprskarova, Martina; Rolcik, Jakub; Latr, Ales; Fischer, Peter M.; Strnad, Miroslav Journal of Medicinal Chemistry, 2006 , vol. 49, # 22 p. 6500 - 6509

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被引用次数: 106

摘要

In a routine screening of our small-molecule compound collection we recently identified 4- arylazo-3, 5-diamino-1 H-pyrazoles as a novel group of ATP antagonists with moderate potency against CDK2-cyclin E. A preliminary SAR study based on 35 analogues suggests ways in which the pharmacophore could be further optimized, for example, via substitutions in the 4-aryl ring. Enzyme kinetics studies with the lead compound and X-ray ...