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

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

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

doi

10.1016/j.ejmech.2014.11.049

subject

Has Abstract

pub_date

2015-01-27 00:00:00

pages

394-405

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)01081-2

journal_volume

90

pub_type

杂志文章

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