Design and synthesis of stable, water soluble radicals as potential anti-cancer agents

Eric Lattmann*, Adiba Begum, M. John Plater

*Corresponding author for this work

Research output: Contribution to journalReview article

Abstract

A free diazafluorenyl radical based on the Koelsch free radical was designed and synthesized with expectations of stability and water solubility. The novel radical precursors were synthesised from the parent brominated stilbene and the substituted fluorenes in an IPSO substitution, as a key synthetic step. The precursors were deprotonated and the anion was discharged by an aqueous solution of potassium cyanoferrate. The new radicals were prepared from fluorene in 6 steps with good overall yields. These radicals have shown promising anticancer activity in initial screenings on 2 different MAC cell lines.

Original languageEnglish
Pages (from-to)195-201
Number of pages7
JournalDrug Design and Discovery
Volume16
Issue number3
Publication statusPublished - 15 Dec 1999

Keywords

  • Anti-cancer agents
  • Koelsch free radical
  • Novel lead structure
  • Stable free radicals
  • Stilbenes
  • Water solubility

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