Recent Patents on Anti-Cancer Drug Discovery

Author(s): Pascale Moreau, Fabrice Anizon, Francis Giraud and Yannick J. Esvan

DOI: 10.2174/1574892811666160519141628

DownloadDownload PDF Flyer Cite As
Heteroaromatic Pim Kinase Inhibitors Containing a Pyrazole Moiety

Page: [309 - 321] Pages: 13

  • * (Excluding Mailing and Handling)

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.