Modifications of the isonipecotic acid fragment of SNS-032: Analogs with improved permeability and lower efflux ratio

Modifications of the isonipecotic acid fragment of SNS-032 results in analogs which are more permeable and lower effluxed than SNS-032. The enantiomerically pure synthesis and the in vivo profile of analog 20 is described.

Graphical abstractThe identification of a selective CDK2, 7, 9 inhibitor 20 with improved permeability is described. The synthesis and in vitro properties of 20 are discussed.Figure optionsDownload full-size imageDownload as PowerPoint slide