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. 2015 Feb 15;25(4):834-40.
doi: 10.1016/j.bmcl.2014.12.068. Epub 2014 Dec 30.

The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors

Hui-Ling Wang  1 , Victor J Cee  2 , Frank Chavez Jr  3 , Brian A Lanman  3 , Anthony B Reed  3 , Bin Wu  3 , Nadia Guerrero  4 , J Russell Lipford  4 , Christine Sastri  4 , Jeff Winston  4 , Kristin L Andrews  5 , Xin Huang  5 , Matthew R Lee  5 , Christopher Mohr  5 , Yang Xu  6 , Yihong Zhou  6 , Andrew S Tasker  3
Affiliations

The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors

Hui-Ling Wang et al. Bioorg Med Chem Lett. .

Abstract

The three Pim kinases are a small family of serine/threonine kinases regulating several signaling pathways that are fundamental to tumorigenesis. As such, the Pim kinases are a very attractive target for pharmacological inhibition in cancer therapy. Herein, we describe our efforts toward the development of a potent, pan-Pim inhibitor. The synthesis and hit-to-lead SAR development from a 3-(pyrazin-2-yl)-1H-indazole derived hit 2 to the identification of a series of potent, pan-Pim inhibitors such as 13o are described.

Keywords: Hematologic malignancy; KMS-12; Multiple myeloma; Pim kinase; pan Pim kinase inhibitor.

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