TY - JOUR
T1 - Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds
AU - Granchi, Carlotta
AU - Calvaresi, Emilia C.
AU - Tuccinardi, Tiziano
AU - Paterni, Ilaria
AU - Macchia, Marco
AU - Martinelli, Adriano
AU - Hergenrother, Paul J.
AU - Minutolo, Filippo
PY - 2013/10/14
Y1 - 2013/10/14
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=84884174877&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84884174877&partnerID=8YFLogxK
U2 - 10.1039/c3ob40870a
DO - 10.1039/c3ob40870a
M3 - Article
C2 - 23986182
AN - SCOPUS:84884174877
SN - 1477-0520
VL - 11
SP - 6588
EP - 6596
JO - Organic and Biomolecular Chemistry
JF - Organic and Biomolecular Chemistry
IS - 38
ER -