Jump to main content
Jump to site search
Access to RSC content Close the message box

Continue to access RSC content when you are not at your institution. Follow our step-by-step guide.


Issue 38, 2013
Previous Article Next Article

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

Author affiliations

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

Back to tab navigation

Supplementary files

Article information


Submitted
26 Apr 2013
Accepted
31 Jul 2013
First published
01 Aug 2013

Org. Biomol. Chem., 2013,11, 6588-6596
Article type
Paper

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

Social activity

Search articles by author

Spotlight

Advertisements