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

• Published in: Ukrainian biochemical journal Vol. 87; no. 3; p. 31
• Main Authors: Kibirev, V K, Osadchuk, T V, Rodik, R V, Kalchenko, V I
• Format: Journal Article
• Language: English
• Published: Ukraine 01.05.2015
• 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
• ISSN: 2409-4943
• DOI: 10.15407/ubj87.03.031

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.