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Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors. 2015
Bin Wu, and
Hui-Ling Wang, and
Victor J Cee, and
Brian A Lanman, and
Thomas Nixey, and
Liping Pettus, and
Anthony B Reed, and
Ryan P Wurz, and
Nadia Guerrero, and
Christine Sastri, and
Jeff Winston, and
J Russell Lipford, and
Matthew R Lee, and
Christopher Mohr, and
Kristin L Andrews, and
Andrew S Tasker
Department of Therapeutic Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320-1799, USA. Electronic address: binw@amgen.com.
PIM kinases are a family of Ser/Thr kinases that are implicated in tumorigenesis. The discovery of a new class of PIM inhibitors, 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines, is discussed with optimized compounds showing excellent potency against all three PIM isoforms.
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