Show simple item record

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

dc.contributor.authorAltamimi, A-MSen_US
dc.contributor.authorAlafeefy, AMen_US
dc.contributor.authorBalode, Aen_US
dc.contributor.authorVozny, Ien_US
dc.contributor.authorPustenko, Aen_US
dc.contributor.authorEl Shikh, MEen_US
dc.contributor.authorAlasmary, FASen_US
dc.contributor.authorAbdel-Gawad, SAen_US
dc.contributor.authorŽalubovskis, Ren_US
dc.date.accessioned2018-02-08T11:36:40Z
dc.date.available2017-11-07en_US
dc.date.issued2018-12en_US
dc.date.submitted2017-12-08T12:53:01.530Z
dc.identifier.urihttp://qmro.qmul.ac.uk/xmlui/handle/123456789/32141
dc.description.abstractA 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).en_US
dc.description.sponsorshipThis project was supported by the National Plan of Science, Technology and Innovation [Grant No. 12-MED2980–54], Prince Sattam bin Abdulaziz University, Alkharj, PO Box 173, 11942.
dc.format.extent147 - 150en_US
dc.languageengen_US
dc.language.isoenen_US
dc.relation.ispartofJ Enzyme Inhib Med Chemen_US
dc.rightsThis is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
dc.subjectLactate dehydrogenaseen_US
dc.subjectinhibitorsen_US
dc.subjecttriazoleen_US
dc.subjectDose-Response Relationship, Drugen_US
dc.subjectEnzyme Inhibitorsen_US
dc.subjectHumansen_US
dc.subjectIsocoumarinsen_US
dc.subjectL-Lactate Dehydrogenaseen_US
dc.subjectMolecular Structureen_US
dc.subjectStructure-Activity Relationshipen_US
dc.subjectTriazolesen_US
dc.titleSymmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A.en_US
dc.typeArticle
dc.rights.holder© 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.
dc.identifier.doi10.1080/14756366.2017.1404593en_US
pubs.author-urlhttps://www.ncbi.nlm.nih.gov/pubmed/29199484en_US
pubs.issue1en_US
pubs.notesNot knownen_US
pubs.publication-statusPublisheden_US
pubs.volume33en_US


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record