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.
Keywords: Biologically active compounds, fused pyrazole, heteroaromatic, non-fused pyrazole, Pim kinase, protein kinase inhibitor.
Recent Patents on Anti-Cancer Drug Discovery
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.
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Moreau Pascale, Anizon Fabrice, Giraud Francis and Esvan J. Yannick, Heteroaromatic Pim Kinase Inhibitors Containing a Pyrazole Moiety, Recent Patents on Anti-Cancer Drug Discovery 2016; 11 (3) . https://dx.doi.org/10.2174/1574892811666160519141628
DOI https://dx.doi.org/10.2174/1574892811666160519141628 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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