Ukr.Biochem.J. 2011; Volume 83, Issue 1, Jan-Feb, pp. 30-37
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.
Keywords: derivatives of 5-amino-1H-pyrazole, furin, inhibitors of furin
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