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Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A.

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).

SUBMITTER: Altamimi AS

PROVIDER: S-EPMC6009863 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature

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Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A.

Altamimi Abdul-Malek S AS Alafeefy Ahmed M AM Balode Agnese A Vozny Igor I Pustenko Aleksandrs A El Shikh Mohey Eldin ME Alasmary Fatmah A S FAS Abdel-Gawad Sherif A SA Žalubovskis Raivis R

Journal of enzyme inhibition and medicinal chemistry 20181201 1

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). ...[more]

PMID: 29199484

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