Synthesis and MMP-2 Inhibition Studies of Novel Aziridine and Azetidine Derivatives

Drug Discovery Conference: Abstract Book 2015
Krista Gulbe, Diāna Stamberga, Andrejs Solops, Ilona Domracheva, Irina Shestakova, Dmitrijs Stepanovs, Māris Turks

Matrix metalloproteinases (MMPs) are zinc-dependent endopeptidases that are responsible for cleavage of extracellular matrix proteins. Because of their effect on both physiological and pathological processes, MMPs have become interesting targets for treatment of cancer. In addition, it is known that MMP-2 has the most important impact to tumor growth. Based on previous research, new series of aziridine and azetidine derivatives containing 1,4-disubstituted 1,2,3-triazole in the side chain as well as aziridine derivatives containing 1,5-disubstituted 1,2,3-triazole in the side chain were synthesized using transition metals catalyzed Huisgen 1,3-dipolar cycloaddition. MMP-2 inhibition studies of target compounds revealed some promising results among aziridine derivatives containing 1,4-disubstituted 1,2,3-triazole, while for other two series inhibition potency was not detected.

Atslēgas vārdi
MMP-2 inhibitors, aziridine-triazole conjugates, azetidine-triazole conjugates

Suta, K., Stamberga, D., Solops, A., Domracheva, I., Shestakova, I., Stepanovs, D., Turks, M. Synthesis and MMP-2 Inhibition Studies of Novel Aziridine and Azetidine Derivatives. No: Drug Discovery Conference: Abstract Book, Latvija, Riga, 27.-29. augusts, 2015. Riga: 2015, 148.-148.lpp.

Publikācijas valoda
English (en)