Synthesis of a potent and selective inhibitor of p90 Rsk.
[reaction: see text] The synthesis of the naturally occurring kaempferol glycoside SL0101 has been accomplished, as has its biochemical evaluation. SL0101 exhibits selective and potent p90 Rsk inhibitory activity at nanomolar concentrations without inhibiting the function of upstream kinases such as MEK, Raf, or PKC. The synthesis verified the structural assignment of the natural product and has provided access to material sufficient for detailed biological evaluation.
Maloney
David J
DJ
Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA.
Hecht
Sidney M
SM
D001578:Benzopyrans / Q000138:chemical synthesis* / Q000494:pharmacology*; D002384:Catalysis; D015394:Molecular Structure; D009005:Monosaccharides / Q000138:chemical synthesis* / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D038744:Ribosomal Protein S6 Kinases, 90-kDa / Q000037:antagonists & inhibitors*
D001578:Benzopyrans; D009005:Monosaccharides; D047428:Protein Kinase Inhibitors; C497449:SL0101; D038744:Ribosomal Protein S6 Kinases, 90-kDa