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Updated: Jul 14, 2026

Solid-phase Synthesis of [4.4] Spirocyclic Oximes
05:15

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Published on: February 6, 2019

Solid-phase synthesis of chlorofusin analogues.

Esther C Y Woon1, Mariangela Arcieri, Andrew F Wilderspin

  • 1Department of Pharmaceutical and Biological Chemistry, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX.

The Journal of Organic Chemistry
|June 15, 2007
PubMed
Summary

We developed a solid-phase synthesis for chlorofusin analogues. These analogues, designed to inhibit the p53/MDM2 interaction, showed no activity, suggesting the complete chromophore is essential.

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Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Molecular Biology

Background:

  • The p53/MDM2 interaction is a critical target for cancer therapy.
  • Chlorofusin analogues are investigated for their potential to modulate this interaction.
  • Developing efficient synthesis methods for these complex molecules is crucial.

Purpose of the Study:

  • To establish a versatile solid-phase synthesis for chlorofusin analogues.
  • To synthesize two distinct series of chlorofusin analogues for biological evaluation.
  • To assess the inhibitory activity of these analogues against the p53/MDM2 interaction.

Main Methods:

  • Solid-phase synthesis utilizing side-chain immobilization.
  • On-resin cyclization and postcyclization modification strategies.
  • Synthesis of chlorofusin analogues with varied chromophores and amino acid substitutions.

Main Results:

  • An efficient and versatile solid-phase synthesis for chlorofusin analogues was successfully developed.
  • Two series of analogues, differing in chromophores and amino acid composition, were synthesized.
  • None of the synthesized analogues demonstrated inhibitory activity against the p53/MDM2 interaction within the tested concentration range.

Conclusions:

  • The developed solid-phase synthesis method is effective for creating diverse chlorofusin analogues.
  • The lack of inhibitory activity suggests that the full chromophore structure of chlorofusin is necessary for p53/MDM2 interaction inhibition.
  • Further studies may be needed to explore analogues with intact chromophore structures.