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J Enzyme Inhib Med Chem ; 33(1): 147-150, 2018 Dec.
Article in English | MEDLINE | ID: mdl-29199484

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).


Subject(s)
Enzyme Inhibitors/pharmacology , Isocoumarins/pharmacology , L-Lactate Dehydrogenase/antagonists & inhibitors , Triazoles/pharmacology , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Humans , Isocoumarins/chemistry , L-Lactate Dehydrogenase/metabolism , Molecular Structure , Structure-Activity Relationship , Triazoles/chemistry
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