Tag Archives: inhibitors of furin
Study on derivatives of 5-amino-4-acylamino-1H-pyrazole as inhibitors of furin
V. K. Kibirev1, T. V. Osadchuk1, O. B. Vadzyuk2,
O. V. Shablykin1, O. P. Kozachenko1, S. A. Chumachenko1,
S. V. Popilnichenko1, V. S. Brovarets1
1Institute of Bioorganic Chemistry and Petrochemistry,
National Academy of Sciences of Ukraine, Kyiv;
е-mail: kibirev@bpci.kiev.ua;
2Palladin Institute of Biochemistry, National Academy
of Sciences of Ukraine, Kyiv
A series of 5-amino-1H-pyrazoles was synthesized and studied as inhibitors of furin. The most potent compound, 5-amino-4-acetylamino-3-(4-methylphenylamino)-1H-pyrazole, was found to retard the activity of furin by mixed-type inhibition with Ki = 288 µМ. These findings permit to plan new ways for chemical modifications of the 5-amino-1H-pyrazole structure and design more potent furin inhibitors of non-peptide nature.
Furin inhibitors based on the derivatives of calix[4]arene CX3im
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.