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...
Saved in:
| Main Authors: | , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English English |
| Published: |
Taylor & Francis
2018
|
| Subjects: | |
| Online Access: | 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 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| Summary: | 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. |
|---|