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

Journal of Enzyme Inhibition and Medicinal Chemistry

Fatmah A. S. Alasmary¹  Ahmed M. Alafeefy²  Abdul-Malek S. Altamimi³  Sherif A. Abdel-Gawad⁴  Mohey Eldin El Shikh⁵  Igor Vozny⁶  Raivis Žalubovskis⁶  Aleksandrs Pustenko⁷  Agnese Balode⁷ 

[1] Chemistry Department, College of Science, King Saud University, Saudi Arabia, Riyadh;Department of Chemistry, Kulliyyah of Science, International Islamic University Malaysia;Department of Pharmaceutical Chemistry, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj, Saudi Arabia;Department of Pharmaceutical Chemistry, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj, Saudi Arabia;Analytical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egyp;Experimental Medicine and Rheumatology, William Harvey Research Institute, Queen Mary University of London, London, UK;Latvian Institute of Organic Synthesis, Riga, Latvia;Latvian Institute of Organic Synthesis, Riga, Latvia;Institute of Technology of Organic Chemistry, Faculty of Materials Science and Applied Chemistry, Riga Technical University, Riga, Latvia;

关键词: Lactate dehydrogenase;    triazole;    inhibitors;   

DOI  :  10.1080/14756366.2017.1404593

来源: publisher

【 摘 要 】

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).

【 授权许可】

CC BY