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

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...

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Autores principales: Altamimi, Abdul-Malek S., Alafeefy, Ahmed M., Balode, Agnese, Vozny, Igor, Pustenko, Aleksandrs, El Shikh, Mohey Eldin, Alasmary, Fatmah A. S., Abdel-Gawad, Sherif A., Žalubovskis, Raivis
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2017
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009863/
https://www.ncbi.nlm.nih.gov/pubmed/29199484
http://dx.doi.org/10.1080/14756366.2017.1404593
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author Altamimi, Abdul-Malek S.
Alafeefy, Ahmed M.
Balode, Agnese
Vozny, Igor
Pustenko, Aleksandrs
El Shikh, Mohey Eldin
Alasmary, Fatmah A. S.
Abdel-Gawad, Sherif A.
Žalubovskis, Raivis
author_facet Altamimi, Abdul-Malek S.
Alafeefy, Ahmed M.
Balode, Agnese
Vozny, Igor
Pustenko, Aleksandrs
El Shikh, Mohey Eldin
Alasmary, Fatmah A. S.
Abdel-Gawad, Sherif A.
Žalubovskis, Raivis
author_sort Altamimi, Abdul-Malek S.
collection PubMed
description 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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spelling pubmed-60098632018-07-11 Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A Altamimi, Abdul-Malek S. Alafeefy, Ahmed M. Balode, Agnese Vozny, Igor Pustenko, Aleksandrs El Shikh, Mohey Eldin Alasmary, Fatmah A. S. Abdel-Gawad, Sherif A. Žalubovskis, Raivis J Enzyme Inhib Med Chem Short Communication 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). Taylor & Francis 2017-12-04 /pmc/articles/PMC6009863/ /pubmed/29199484 http://dx.doi.org/10.1080/14756366.2017.1404593 Text en © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This 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.
spellingShingle Short Communication
Altamimi, Abdul-Malek S.
Alafeefy, Ahmed M.
Balode, Agnese
Vozny, Igor
Pustenko, Aleksandrs
El Shikh, Mohey Eldin
Alasmary, Fatmah A. S.
Abdel-Gawad, Sherif A.
Žalubovskis, Raivis
Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
title Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
title_full Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
title_fullStr Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
title_full_unstemmed Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
title_short Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
title_sort symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-a
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6009863/
https://www.ncbi.nlm.nih.gov/pubmed/29199484
http://dx.doi.org/10.1080/14756366.2017.1404593
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