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

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Publikācijas valoda English (en)
Nosaukums oriģinālvalodā Discovery of Aziridine–Triazole Conjugates as Selective MMP-2 Inhibitors
Pētniecības nozare 1. Dabaszinātnes
Pētniecības apakšnozare 1.4. Ķīmija
Autori Imants Kreituss
Elīna Rozenberga
Jānis Zemītis
Peteris Trapencieris
Nadezhda Romanchikova
Māris Turks
Atslēgas vārdi aziridines, aziridine–triazole conjugates, triazoles, anticancer drugs, azide-alkyne dipolar cycloaddition, MMP-2 inhibitors
Anotācija 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
Hipersaite: http://link.springer.com/article/10.1007%2Fs10593-013-1351-9 
Atsauce 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, 1191.-1200.lpp. ISSN 0009-3122. Pieejams: doi:10.1007/s10593-013-1351-9
Papildinformācija Citējamību skaits:
ID 16445