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

Altamimi AS 1 , Alafeefy AM 2 , Balode A 3 , Vozny I 3 , Pustenko A 3 , El Shikh ME 4 Show all authors , Alasmary FAS 5 , Abdel-Gawad SA 1 , Žalubovskis R 3

Affiliations 

  • 1 a Department of Pharmaceutical Chemistry, College of Pharmacy , Prince Sattam Bin Abdulaziz University , Alkharj , Saudi Arabia
  • 2 b Department of Chemistry , Kulliyyah of Science, International Islamic University Malaysia
  • 3 c Latvian Institute of Organic Synthesis , Riga , Latvia
  • 4 e Experimental Medicine and Rheumatology , William Harvey Research Institute, Queen Mary University of London , London , UK
  • 5 f Chemistry Department, College of Science , King Saud University , Saudi Arabia , Riyadh
J Enzyme Inhib Med Chem, 2018 Dec;33(1):147-150.
PMID: 29199484 DOI: 10.1080/14756366.2017.1404593

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).

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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