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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Heteroaromatic Pim Kinase Inhibitors Containing a Pyrazole Moiety
Pascale Moreau1, Fabrice Anizon, Francis Giraud
1Clermont Université, Université Blaise Pascal, Institut de Chimie de Clermont-Ferrand (ICCF) - UMR CNRS 6296, 24 avenue Blaise Pascal, TSA 60026, CS 60026, 63178 Aubière Cedex, France. Pascale.MOREAU@univ-bpclermont.fr.
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.
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