Benzo[c][2,7]naphthyridines as inhibitors of PDK-1

A series of substituted benzo[c][2,7]-naphthyridines were prepared and showed good potency in inhibiting PDK-1. The synthesis and SAR of this series of compounds are presented as well as the X-ray crystal structure of one of these analogs in a complex with PDK-1.

Graphical abstractThe synthesis and structure–activity relationships for a series of benzo[c][2,7]naphthyridines as inhibitors of PDK-1 are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide