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

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. Published by Elsevier Ltd.

Citation

Hui-Ling Wang, Victor J Cee, Frank Chavez, Brian A Lanman, Anthony B Reed, Bin Wu, Nadia Guerrero, J Russell Lipford, Christine Sastri, Jeff Winston, Kristin L Andrews, Xin Huang, Matthew R Lee, Christopher Mohr, Yang Xu, Yihong Zhou, Andrew S Tasker. The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors. Bioorganic & medicinal chemistry letters. 2015 Feb 15;25(4):834-40

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PMID: 25597005

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