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      Three acetylated flavonol glycosides from Forsteronia refracta that specifically inhibit p90 RSK.

      Bioorganic & Medicinal Chemistry
      Acetylation, Apocynaceae, chemistry, Enzyme Inhibitors, pharmacology, Flavonols, Glycosides, Molecular Structure, Plant Extracts, isolation & purification, Ribosomal Protein S6 Kinases, 90-kDa, antagonists & inhibitors, Species Specificity, Stereoisomerism

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          Abstract

          A survey of plant extracts for the presence of p90 ribosomal S6 kinase (RSK) inhibitors resulted in the isolation of three acetylated flavonol glycosides. Kaempferol 3-O-(2'',4''-O-diacetyl-alpha-l-rhamnopyranoside) (1), kaempferol 3-O-(3'',4''-O-diacetyl-alpha-l-rhamnopyranoside) (2), and kaempferol-3-O-(4''-O-acetyl-alpha-l-rhamnopyranoside) (3) were isolated from Forsteronia refracta as the first RSK inhibitors. Of these, compound 2 was found to be the best inhibitor with an IC(50) value of 89 nM.

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