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).

Atslēgas vārdi
Lactate dehydrogenase; triazole; inhibitors
DOI
10.1080/14756366.2017.1404593
Hipersaite
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, 147.-150.lpp. ISSN 1475-6366. e-ISSN 1475-6374. Pieejams: doi:10.1080/14756366.2017.1404593

Publikācijas valoda
English (en)