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

Altamimi, Abdul Malek S. and Alafeefy, Ahmed Mahmoud and Balode, Agnese and Vozny, Igor V. and Pustenko, Aleksandrs and El Shikh, Mohey Eldin M. and Alasmary, Fatmah Ali S. and Abdel-Gawad, Sherif A. and Žalubovskis, Raivis (2018) Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A. Journal of Enzyme Inhibition and Medicinal Chemistry, 33 (1). pp. 147-150. ISSN 1475-6366 E-ISSN 1475-6374 (In Press)

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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). © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.

Item Type:	Article (Journal)
Additional Information:	7668/65282
Uncontrolled Keywords:	InhibitorsLactate; Dehydrogenase; Triazole
Subjects:	Q Science > QC Physics
Kulliyyahs/Centres/Divisions/Institutes (Can select more than one option. Press CONTROL button):	Kulliyyah of Science Kulliyyah of Science > Department of Physics
Depositing User:	Dr Ahmed Alafeefy
Date Deposited:	27 Jun 2019 08:35
Last Modified:	27 Jun 2019 08:35
URI:	http://irep.iium.edu.my/id/eprint/65282

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