TY - JOUR
T1 - Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A
AU - Sherif A., Abdul Malek S.
AU - Alafeefy, Ahmed M.
AU - Balode, Agnese
AU - Vozny, Igor
AU - Pustenko, Aleksandrs
AU - El Shikh, Mohey Eldin
AU - Alasmary, Fatmah A.S.
AU - Sherif A., Abdel Malek
AU - Žalubovskis, Raivis
N1 - Publisher Copyright:
© 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.
PY - 2018/1/1
Y1 - 2018/1/1
N2 - 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).
AB - 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).
KW - inhibitors
KW - Lactate dehydrogenase
KW - triazole
UR - https://www.scopus.com/pages/publications/85038351577
U2 - 10.1080/14756366.2017.1404593
DO - 10.1080/14756366.2017.1404593
M3 - Article
C2 - 29199484
AN - SCOPUS:85038351577
SN - 1475-6366
VL - 33
SP - 147
EP - 150
JO - Journal of Enzyme Inhibition and Medicinal Chemistry
JF - Journal of Enzyme Inhibition and Medicinal Chemistry
IS - 1
ER -
