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.
|Autori:||Carlotta Granchi; Emilia C. Calvaresi; Tiziano Tuccinardi; Ilaria Paterni; Marco Macchia; Adriano Martinelli; Paul J. Hergenrother; Filippo Minutolo|
|Titolo:||Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds|
|Anno del prodotto:||2013|
|Digital Object Identifier (DOI):||10.1039/C3OB40870A|
|Appare nelle tipologie:||1.1 Articolo in rivista|