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 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.

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

GRANCHI, CARLOTTA;TUCCINARDI, TIZIANO;PATERNI, ILARIA;MACCHIA, MARCO;MARTINELLI, ADRIANO;MINUTOLO, FILIPPO
2013

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 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.
Granchi, Carlotta; Emilia C., Calvaresi; Tuccinardi, Tiziano; Paterni, Ilaria; Macchia, Marco; Martinelli, Adriano; Paul J., Hergenrother; Minutolo, Filippo
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/226342
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