Synthesis of a Potent and Selective Inhibitor of p90 Rsk

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. Th...

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Bibliographic Details
Published inOrganic letters Vol. 7; no. 6; pp. 1097 - 1099
Main Authors Maloney, David J, Hecht, Sidney M
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 17.03.2005
Amer Chemical Soc
Subjects
Benzopyrans - chemical synthesis
Benzopyrans - pharmacology
Catalysis
Chemistry
Chemistry, Organic
Molecular Structure
Monosaccharides - chemical synthesis
Monosaccharides - pharmacology
Physical Sciences
Protein Kinase Inhibitors - chemical synthesis
Protein Kinase Inhibitors - pharmacology
Ribosomal Protein S6 Kinases, 90-kDa - antagonists & inhibitors
Science & Technology
SIGNAL-TRANSDUCTION
BREAST-CANCER CELLS
ERBB-2
DIMETHYLDIOXIRANE
PATHWAY
EPOXIDATION
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Summary: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.
Bibliography:Medline
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ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:1523-7060
1523-7052
DOI:10.1021/ol0500463