title: Heteroaromatic Pim Kinase Inhibitors Containing a Pyrazole Moiety.
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.
authors.affiliation: Clermont 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.
authors.forename: Pascale
authors.initials: P
authors.lastname: Moreau
authors.forename: Fabrice
authors.initials: F
authors.lastname: Anizon
authors.forename: Francis
authors.initials: F
authors.lastname: Giraud
authors.forename: Yannick J
authors.initials: YJ
authors.lastname: Esvan
mesh_terms: D000818:Animals; D055808:Drug Discovery; D006801:Humans; D008958:Models, Molecular; D058990:Molecular Targeted Therapy; D011487:Protein Conformation; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D051573:Proto-Oncogene Proteins c-pim-1 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology*; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D051573:Proto-Oncogene Proteins c-pim-1; C406031:proto-oncogene proteins pim