Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors

A series of four bicyclic cores were prepared and evaluated as cyclin-dependent kinase-2 (CDK2) inhibitors. From the in-vitro and cell-based analysis, the pyrazolo[1,5-a]pyrimidine core (represented by 9) emerged as the superior core for further elaboration in the identification of novel CDK2 inhibitors.

Graphical abstractPyrazolo[1,5-a]pyrimidine 9 emerged as a key template for further optimization toward the identification of CDK inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide