The 90 kDa ribosomal S6 kinase (RSK) family of proteins is a highly conserved group of serine/threonine protein kinases that regulate cell growth, cell motility, cell survival and cell proliferation.  RSK1, one of four human isoforms, is amplified in breast and prostate tumors and implicated in other human diseases.  We report here a novel series of [1,2,4]triazolo[1,5-a]pyridines, identified through structure based optimization of a high throughput screening hit, that are potent and selective RSK inhibitors.  Synthesis, SAR, and x-ray crystallographic analysis for this series will be described.

Discovery and SAR exploration of a novel series of [1,2,4]triazolo[1,5-a]pyridines as potent and selective RSK inhibitors

246th National Meeting (2013)

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