4.7 Article

Synthesis and Biological Evaluation of 4′-Substituted Kaempfer-3-ols

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 85, Issue 6, Pages 4279-4288

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.9b03461

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Funding

  1. National Science Foundation [CHE-1565788]
  2. National Institutes of Health [AI146485, AI144196, AI142040, CA213201]

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The synthesis of two series of five kaempfer-3-ols was described. The first set all have a C-3 hydroxyl group and the second has a carboxymethoxy ether at the C-3 position. Both series have variable substitution at the C-4' position (i.e., OH, CI, F, H, OMe). Both kaempferols and carboxymethoxy ethers were evaluated for their ability to inhibit ribosomal s6 kinase (RSK) activity and cancer cell proliferation.

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