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

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...

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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2017
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009863/
https://www.ncbi.nlm.nih.gov/pubmed/29199484
http://dx.doi.org/10.1080/14756366.2017.1404593
Descripción
Sumario: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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