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ID: ALA1156062

Journal: Bioorg Med Chem Lett

Title: Synthesis, SAR, and X-ray structure of tricyclic compounds as potent FBPase inhibitors.

Authors: Tsukada T, Takahashi M, Takemoto T, Kanno O, Yamane T, Kawamura S, Nishi T.

Abstract: With the aim of discovering a novel class of fructose-1,6-bisphosphatase (FBPase) inhibitors, a series of compounds based on tricyclic scaffolds was synthesized. Extensive SAR studies led to the finding of 8l with an IC50 value of 0.013 microM against human FBPase. An X-ray crystallographic study revealed that 8l bound at AMP binding sites of human liver FBPase with hydrogen bonding interactions similar to AMP.

CiteXplore: 19762234

DOI: 10.1016/j.bmcl.2009.08.081