1380911-90-9Relevant academic research and scientific papers
The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors
Wang, Hui-Ling,Cee, Victor J.,Chavez, Frank,Lanman, Brian A.,Reed, Anthony B.,Wu, Bin,Guerrero, Nadia,Lipford, J. Russell,Sastri, Christine,Winston, Jeff,Andrews, Kristin L.,Huang, Xin,Lee, Matthew R.,Mohr, Christopher,Xu, Yang,Zhou, Yihong,Tasker, Andrew S.
, p. 834 - 840 (2015/02/19)
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.
BICYCLIC COMPOUNDS AS PIM INHIBITORS
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Page/Page column 110-111, (2012/06/30)
The invention relates to bicyclic compounds of formula (1'), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
