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

具有1,4-三唑部分的对称分子是肿瘤相关乳酸脱氢酶-A的强效抑制剂。

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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 IC(50) = 117-174 µM. Seven compounds exhibited better LDHA inhibition (IC(50) 117-136 µM) compared to known LDH inhibitor - galloflavin (IC(50) 157 µM).

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