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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

Carlotta Granchi, Emilia C Calvaresi, Tiziano Tuccinardi, Ilaria Paterni, Marco Macchia, Adriano Martinelli, Paul J Hergenrother, Filippo Minutolo

Org Biomol Chem. 2013 Oct 14;11(38):6588-96.

PMID: 23986182

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1269802972 NHI-2 NHI-2 1269802-97-2 Price
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