Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A.
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J Enzyme Inhib Med Chem
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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 220.127.116.11) 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).
AuthorsAltamimi, A-MS; Alafeefy, AM; Balode, A; Vozny, I; Pustenko, A; El Shikh, ME; Alasmary, FAS; Abdel-Gawad, SA; Žalubovskis, R
- Inflammation