Title:Heteroaromatic Pim Kinase Inhibitors Containing a Pyrazole Moiety
Volume: 11
Issue: 3
Author(s): Pascale Moreau, Fabrice Anizon, Francis Giraud and Yannick J. Esvan
Affiliation:
Keywords:
Biologically active compounds, fused pyrazole, heteroaromatic, non-fused pyrazole, Pim kinase, protein kinase
inhibitor.
Abstract: This review, of the literature published between 2010 and 2015 reports that molecules containing
a non-fused and/or fused pyrazole moiety could exhibit very potent activity toward Pim
kinases, including the inhibition of cellular Bad phosphorylation as well as antiproliferative activity
against various cancer cells. Even if Pim kinase inhibitors currently in clinical trial do not exhibit a
pyrazole moiety, heteroaromatic kinase inhibitors containing an indazole part such as Axitinib and Pazopanib
already reached the market. Therefore, one can imagine that in the future, heteroaromatic derivatives
inhibiting Pim kinases including pyrazoles could be identified and used for their diagnostic and/or therapeutic
potential alone or in combination with other drugs for the diseases in which Pim kinases are involved.
