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. 2015 Feb 15;25(4):775-80.
doi: 10.1016/j.bmcl.2014.12.091. Epub 2015 Jan 7.

Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors

Bin Wu  1 , Hui-Ling Wang  2 , Victor J Cee  2 , Brian A Lanman  2 , Thomas Nixey  2 , Liping Pettus  2 , Anthony B Reed  2 , Ryan P Wurz  2 , Nadia Guerrero  3 , Christine Sastri  3 , Jeff Winston  3 , J Russell Lipford  3 , Matthew R Lee  4 , Christopher Mohr  4 , Kristin L Andrews  4 , Andrew S Tasker  2
Affiliations

Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors

Bin Wu et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: 1,3,4-Thiadiazol-2-amines; Kinase inhibitors; Lead optimization; PIM kinases.

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