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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Main Authors: Altamimi, Abdul Malek S., Alafeefy, Ahmed Mahmoud, Balode, Agnese, Vozny, Igor V., Pustenko, Aleksandrs, El Shikh, Mohey Eldin M., Alasmary, Fatmah Ali S., Abdel-Gawad, Sherif A., Žalubovskis, Raivis
Format: Article
Language:English
English
Published: Taylor & Francis 2018
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Online Access:http://irep.iium.edu.my/65282/
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http://irep.iium.edu.my/65282/
http://irep.iium.edu.my/65282/1/65282_Symmetric%20molecules%20with%201%2C4-triazole%20moieties%20_article.pdf
http://irep.iium.edu.my/65282/2/65282_Symmetric%20molecules%20with%201%2C4-triazole%20moieties%20_scopus.pdf
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spelling iium-652822019-06-27T00:35:26Z http://irep.iium.edu.my/65282/ Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A Altamimi, Abdul Malek S. Alafeefy, Ahmed Mahmoud Balode, Agnese Vozny, Igor V. Pustenko, Aleksandrs El Shikh, Mohey Eldin M. Alasmary, Fatmah Ali S. Abdel-Gawad, Sherif A. Žalubovskis, Raivis QC Physics 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. Taylor & Francis 2018-01-01 Article PeerReviewed application/pdf en http://irep.iium.edu.my/65282/1/65282_Symmetric%20molecules%20with%201%2C4-triazole%20moieties%20_article.pdf application/pdf en http://irep.iium.edu.my/65282/2/65282_Symmetric%20molecules%20with%201%2C4-triazole%20moieties%20_scopus.pdf 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) https://www.tandfonline.com/doi/full/10.1080/14756366.2017.1404593 10.1080/14756366.2017.1404593
repository_type Digital Repository
institution_category Local University
institution International Islamic University Malaysia
building IIUM Repository
collection Online Access
language English
English
topic QC Physics
spellingShingle QC Physics
Altamimi, Abdul Malek S.
Alafeefy, Ahmed Mahmoud
Balode, Agnese
Vozny, Igor V.
Pustenko, Aleksandrs
El Shikh, Mohey Eldin M.
Alasmary, Fatmah Ali S.
Abdel-Gawad, Sherif A.
Žalubovskis, Raivis
Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
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 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.
format Article
author Altamimi, Abdul Malek S.
Alafeefy, Ahmed Mahmoud
Balode, Agnese
Vozny, Igor V.
Pustenko, Aleksandrs
El Shikh, Mohey Eldin M.
Alasmary, Fatmah Ali S.
Abdel-Gawad, Sherif A.
Žalubovskis, Raivis
author_facet Altamimi, Abdul Malek S.
Alafeefy, Ahmed Mahmoud
Balode, Agnese
Vozny, Igor V.
Pustenko, Aleksandrs
El Shikh, Mohey Eldin M.
Alasmary, Fatmah Ali S.
Abdel-Gawad, Sherif A.
Žalubovskis, Raivis
author_sort Altamimi, Abdul Malek S.
title 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_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_sort symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-a
publisher Taylor & Francis
publishDate 2018
url http://irep.iium.edu.my/65282/
http://irep.iium.edu.my/65282/
http://irep.iium.edu.my/65282/
http://irep.iium.edu.my/65282/1/65282_Symmetric%20molecules%20with%201%2C4-triazole%20moieties%20_article.pdf
http://irep.iium.edu.my/65282/2/65282_Symmetric%20molecules%20with%201%2C4-triazole%20moieties%20_scopus.pdf
first_indexed 2023-09-18T21:32:39Z
last_indexed 2023-09-18T21:32:39Z
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