Symmetric molecules with 1, 4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A. (1st January 2018)

• Record Type: Journal Article
• Authors: Altamimi, Abdul-Malek S.; Alafeefy, Ahmed M.; Balode, Agnese; Vozny, Igor; Pustenko, Aleksandrs; El Shikh, Mohey Eldin; Alasmary, Fatmah A. S.; Abdel-Gawad, Sherif A.; Žalubovskis, Raivis
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 33:Number 1(2018)
• Page Start: 147
• Page End: 150
• Publication Date: 2018-01-01
• Subjects: Lactate dehydrogenase -- triazole -- inhibitors; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.1080/14756366.2017.1404593
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract: A series of symmetric molecules incorporating aryl or pyridyl moieties as central core and 1, 4-substituted triazoles as a side bridge was synthesised. The new compounds were investigated as lactate dehydro-genase (LDH, EC 1.1.1.27) inhibitors. The cancer associated LDHA isoform was inhibited with IC50 = 117–174 µM. Seven compounds exhibited better LDHA inhibition (IC50 117–136 µM) compared to known LDH inhibitor – galloflavin (IC50 157 µM).