Heteroaromatic Pim Kinase Inhibitors Containing a Pyrazole Moiety

被引:8
作者
Moreau, Pascale
Anizon, Fabrice
Giraud, Francis
Esvan, Yannick J.
机构
[1] Univ Clermont Ferrand, Univ Clermont Auvergne, Inst Chim Clermont Ferrand, BP 10448, F-63000 Clermont Ferrand, France
[2] ICCF, CNRS, UMR 6296, F-63178 Aubiere, France
关键词
Biologically active compounds; fused pyrazole; heteroaromatic; non-fused pyrazole; Pim kinase; protein kinase inhibitor; DISCOVERY; POTENT; IDENTIFICATION; DESIGN; CANCER; OPTIMIZATION; DERIVATIVES; SITE; HIT;
D O I
10.2174/1574892811666160519141628
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
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.
引用
收藏
页码:309 / 321
页数:13
相关论文
共 65 条
[61]   Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design [J].
Wang, Xiaojing ;
Magnuson, Steven ;
Pastor, Rich ;
Fan, Eric ;
Hu, Huiyong ;
Tsui, Vickie ;
Deng, Wei ;
Murray, Jeremy ;
Steffek, Micah ;
Wallweber, Heidi ;
Moffat, John ;
Drummond, Jason ;
Chan, Grace ;
Harstad, Eric ;
Ebens, Allen J. .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (11) :3149-3153
[62]   PIM kinase (and Akt) biology and signaling in tumors [J].
Warfel, Noel A. ;
Kraft, Andrew S. .
PHARMACOLOGY & THERAPEUTICS, 2015, 151 :41-49
[63]  
Xu Y, 2013, Preparation of imidazo [1,2-b] pyridazine, pyrazolo[1,5-a] pyrimidine, and [1,2,4] triazolo[4,3-a] pyridine derivatives as protein kinase inhibitors, Patent No. [WO 2013013188, 2013013188]
[64]   Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors [J].
Xu, Yong ;
Brenning, Benjamin G. ;
Kultgen, Steven G. ;
Foulks, Jason M. ;
Clifford, Adrianne ;
Lai, Shuping ;
Chan, Ashley ;
Merx, Shannon ;
McCullar, Michael V. ;
Kanner, Steven B. ;
Ho, Koc-Kan .
ACS MEDICINAL CHEMISTRY LETTERS, 2015, 6 (01) :63-67
[65]  
Xue C. B., 2014, Patent No. [WO2014113388, 2014113388]