Discovery of novel indole derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase.

Basic Information

ID: ALA3392954

Journal: Eur J Med Chem

Title: Discovery of novel indole derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase.

Authors: Bie J, Liu S, Li Z, Mu Y, Xu B, Shen Z.

Abstract: A series of novel indole derivatives was designed and synthesized as inhibitors of fructose-1,6-bisphosphatase (FBPase). The most potent compound 14c was identified with an IC50 value of 0.10 μM by testing the inhibitory activity against recombinant human FBPase. The structure-activity relationships were investigated on the substitution at 4- and 5-position of the indole scaffold. The binding interactions of the title compounds at AMP binding site of FBPase were predicted using CDOCKER algorithm.

CiteXplore: 25461330

DOI: 10.1016/j.ejmech.2014.11.049

Patent ID: