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Publikācija: Discovery of Aziridine–Triazole Conjugates as Selective MMP-2 Inhibitors

Publication Type Scientific article indexed in SCOPUS or WOS database
Funding for basic activity Unknown
Defending: ,
Publication language English (en)
Title in original language Discovery of Aziridine–Triazole Conjugates as Selective MMP-2 Inhibitors
Field of research 1. Natural sciences
Sub-field of research 1.4 Chemical sciences
Authors Imants Kreituss
Elīna Rozenberga
Jānis Zemītis
Peteris Trapencieris
Nadezhda Romanchikova
Māris Turks
Keywords aziridines, aziridine–triazole conjugates, triazoles, anticancer drugs, azide-alkyne dipolar cycloaddition, MMP-2 inhibitors
Abstract A series of (aryltriazolyl)methylaziridines were synthesized and evaluated as selective inhibitors of matrix metalloproteinase-2. They constitute a novel class of hydroxamic acid-free matrix metalloproteinase inhibitors. The triazole fragment serves as a linker between the hydrophilic aziridine and the lipophilic part of the molecule. The best inhibition was observed with 1-(aziridin-2-ylmethyl)-4-(4-butylphenyl)-1H-1,2,3-triazole and 1-(aziridin-2-ylmethyl)-4-phenyl-1H-1,2,3-triazole that selectively inhibited MMP-2 at 73% in 20 μM concentration and at 75% in 10 μM concentration, respectively.
DOI: 10.1007/s10593-013-1351-9
Hyperlink: http://link.springer.com/article/10.1007%2Fs10593-013-1351-9 
Reference Kreituss, I., Rozenberga, E., Zemītis, J., Trapencieris, P., Romanchikova, N., Turks, M. Discovery of Aziridine–Triazole Conjugates as Selective MMP-2 Inhibitors. Chemistry of Heterocyclic Compounds, 2013, Vol.49, Iss.8, pp.1191-1200. ISSN 0009-3122. Available from: doi:10.1007/s10593-013-1351-9
Additional information Citation count:
ID 16445