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Biological Activity:
The first GTP-competitive inhibitor of human cytosolic phosphoenolpyruvate carboxykinase (PEPCK or cPEPCK) with low submicormolar IC50 values.
References:
LH Foley et al. Modified 3-alkyl-1,8-dibenzylxanthines as GTP-competitive inhibitors of phosphoenolpyruvate carboxykinase. Bioorg Med Chem Lett. 2003, 13(20), 3607-10. [online]
LH Foley et al. X-ray structures of two xanthine inhibitors bound to PEPCK and N-3 modifications of substituted 1,8-dibenzylxanthines. Bioorg Med Chem Lett. 2003, 13(21), 3871-4. [online]
SL Pietranico et al. C-8 Modifications of 3-alkyl-1,8-dibenzylxanthines as inhibitors of human cytosolic phosphoenolpyruvate carboxykinase. Bioorg Med Chem Lett. 2007, 17(14), 3835-9. [online]
Chemical Name: N-{4-[3-Butyl-1-(2-fluoro-benzyl)-2,6-dioxo-2,3,6,9-tetrahydro-1H-purin-8-ylmethyl]-phenyl}-acetamide
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