Clear Search sequence regions


  • activity (1)
  • humans (1)
  • indazoles (3)
  • Pim (8)
  • Sizes of these terms reflect their relevance to your search.

    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

    Expand section icon Mesh Tags

    Expand section icon Substances


    PMID: 25597005

    View Full Text