Ukr.Biochem.J. 2015; Volume 87, Issue 3, May-Jun, pp. 31-36

doi: https://doi.org/10.15407/ubj87.03.031

Furin inhibitors based on the derivatives of calix[4]arene CX3im

08.07.2015   Uncategorized   No comments

V. K. Kibirev1, T. V. Osadchuk2, R. V. Rodik3, V. I. Kalchenko3

1Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine, Kyiv;
e-mail: kibirev@biochem.kiev.ua;
2Institute of Bioorganic Chemistry and Petrochemistry, National Academy
of Sciences of Ukraine, Kyiv;
3Institute of Organic Chemistry, National Academy of Sciences of Ukraine, Kyiv

The aim of this work was to study antifurin activity of some derivatives of calix[4]arenes modified on the upper rim of the macrocycle by positively charged or uncharged groups. It was found that calixarene CX3im­ derivatives containing positively charged N-methylimidazolium cycles were indeed able to inhibit furin (Ki = 58.2 μM). The magnitude of the effects depended also on the hydrophobicity of the substituents located on the lower rim of the macrocycle. The  findings indicated the possibility of creating furin inhibitors of new generation based on the calix[4]arene platform.

Keywords: , ,

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