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Synlett 1995; 1995(SI): 533-535
DOI: 10.1055/s-1995-5288
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On the Protein Kinase C Pharmacophore: Synthesis and Biological Activity of 4-Hydroxylated Analogs of Ingenol

Jeffrey D. Winkler1 , Bor-Cherng Hong, Sanghee Kim, Nancy E. Lewin, Peter M. Blumberg2
  • 1Department of Chemistry, The University of Pennsylvania, Philadelphia, Pennsylvania 19104
  • 2Molecular Mechanism of Tumor Promotion Section, Laboratory of Cellular Carcinogenesis and Tumor Promotion, National Cancer Institute, Bethesda, Maryland 20892
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Publication Date:
31 December 2000 (online)

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The synthesis and preliminary biological evaluation of the first C-4 hydroxylated analog of ingenol are described. The activity of 4 demonstrates that the C-4 hydroxyl group is not a critical component of the pharmacophore for protein kinase C binding and activation.

ingenol - protein kinase C - pharmacophore - structure-activity relationships