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

Abdul-Malek S. Altamimi; Ahmed M. Alafeefy; Agnese Balode; Igor Vozny; Aleksandrs Pustenko; Mohey Eldin El Shikh; Fatmah A. S. Alasmary; Sherif A. Abdel-Gawad; Raivis Žalubovskis

doi:10.1080/14756366.2017.1404593

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

Journal article

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

Abdul-Malek S. Altamimi, Ahmed M. Alafeefy, Agnese Balode, Igor Vozny, Aleksandrs Pustenko, Mohey Eldin El Shikh, Fatmah A. S. Alasmary, Sherif A. Abdel-Gawad and Raivis Žalubovskis

Journal of enzyme inhibition and medicinal chemistry, Vol.33(1), pp.147-150

01/01/2018

DOI: https://doi.org/10.1080/14756366.2017.1404593

PMCID: PMC6009863

PMID: 29199484

Abstract

inhibitors

Lactate dehydrogenase

Short Communication

triazole

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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Title: Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
Creators - without role: Abdul-Malek S. Altamimi - Prince Sattam Bin Abdulaziz University
Ahmed M. Alafeefy - International Islamic University Malaysia
Agnese Balode - Riga Technical University
Igor Vozny - Latvijas Organiskās Sintēzes Institūts
Aleksandrs Pustenko - Riga Technical University
Mohey Eldin El Shikh - Queen Mary University of London
Fatmah A. S. Alasmary - King Saud University
Sherif A. Abdel-Gawad - Cairo University
Raivis Žalubovskis - Latvijas Organiskās Sintēzes Institūts
Publication Details: Journal of enzyme inhibition and medicinal chemistry, Vol.33(1), pp.147-150
Publisher: Taylor & Francis
Grant note: ; ; 12-; –54 / ;
Identifiers: 9925564408331
Academic Unit: Prince Sattam Bin Abdulaziz University
Language: English
Resource Type: Journal article