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Issue 38, 2013
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Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds

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Abstract

A head-to-head study of representative examples of N-hydroxyindole-2-carboxylates (NHI) and malonic derivatives (Mal) as LDH-A inhibitors was conducted, comparing the enzyme inhibition potency, cellular uptake, reduction of lactate production in cancer cells and anti-proliferative activity. Among the compounds tested, methyl 1-hydroxy-6-phenyl-4-(trifluoromethyl)-1H-indole-2-carboxylate (2, NHI-2), a methyl ester belonging to the NHI class, displayed optimal properties in the cell-based assays, proving to be an efficient anti-glycolytic agent against cancer cells.

Graphical abstract: Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds

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Publication details

The article was received on 26 Apr 2013, accepted on 31 Jul 2013 and first published on 01 Aug 2013


Article type: Paper
DOI: 10.1039/C3OB40870A
Citation: Org. Biomol. Chem., 2013,11, 6588-6596
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    Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds

    C. Granchi, E. C. Calvaresi, T. Tuccinardi, I. Paterni, M. Macchia, A. Martinelli, P. J. Hergenrother and F. Minutolo, Org. Biomol. Chem., 2013, 11, 6588
    DOI: 10.1039/C3OB40870A

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