Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: A template-based approach

The synthesis and hit-to-lead SAR development from a pyrazolo[1,5-a]pyrimidine-derived hit 5 to the identification of a series of potent, pan–Pim inhibitors such as 11j are described.

Graphical abstractThe synthesis and SAR development of a class of pyrazolo[1,5-a]pyrimidine-based Pim kinase inhibitors are detailed from an early HTS hit to a pan–Pim inhibitor such as 11j.Figure optionsDownload full-size imageDownload as PowerPoint slide