FURIN INHIBITORS BASED ON THE DERIVATIVES OF CALIX[4]ARENE CX3im

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 t...

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Bibliographic Details
Published in:Ukrainian biochemical journal 2015-05, Vol.87 (3), p.31-36
Main Authors: Kibirev, V K, Osadchuk, T V, Rodik, R V, Kalchenko, V I
Format: Article
Language:English
Subjects:
Calixarenes - chemical synthesis
Calixarenes - chemistry
Calixarenes - pharmacology
Dose-Response Relationship, Drug
Drug Design
Furin - antagonists & inhibitors
Hydrogen-Ion Concentration
Molecular Structure
Protease Inhibitors - chemical synthesis
Protease Inhibitors - chemistry
Protease Inhibitors - pharmacology
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Summary: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 (K(i) = 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.
ISSN:2409-4943
DOI:10.15407/ubj87.03.031