Symmetric Molecules with 1,4-Triazole Moieties as Potent Inhibitors of Tumour-Associated Lactate Dehydrogenase-A
Journal of Enzyme Inhibition and Medicinal Chemistry
2018
Abdul-Malek Altamimi,
Ahmed Alafeefy,
Agnese Balode,
Igor Vozny,
Aleksandrs Pustenko,
Mohey Eldin Shikh,
Fatmah Alasmary,
Sherif Abdel-Gawad,
Raivis Žalubovskis
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 ¼117–174mM. Seven compounds exhibited better LDHA inhibition (IC 50 117–136mM) compared to known LDH inhibitor–galloflavin (IC 50 157mM).
Keywords
Lactate dehydrogenase; triazole; inhibitors
DOI
10.1080/14756366.2017.1404593
Hyperlink
http://www.tandfonline.com/doi/full/10.1080/14756366.2017.1404593
Altamimi, A., Alafeefy, A., Balode, A., Vozny, I., Pustenko, A., Shikh, M., Alasmary, F., Abdel-Gawad, S., Žalubovskis, R. Symmetric Molecules with 1,4-Triazole Moieties as Potent Inhibitors of Tumour-Associated Lactate Dehydrogenase-A. Journal of Enzyme Inhibition and Medicinal Chemistry, 2018, Vol. 33, No. 1, pp.147-150. ISSN 1475-6366. e-ISSN 1475-6374. Available from: doi:10.1080/14756366.2017.1404593
Publication language
English (en)