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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2018
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my.iium.irep.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 (In Press) https://www.tandfonline.com/doi/full/10.1080/14756366.2017.1404593 10.1080/14756366.2017.1404593 |
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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 |
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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. |
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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/65282/1/65282_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 http://irep.iium.edu.my/65282/ https://www.tandfonline.com/doi/full/10.1080/14756366.2017.1404593 |
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1643619729915510784 |