Antineoplastic agents 463. Synthesis of combretastatin A-3 diphosphate prodrugs

George Pettit, M. D. Minardi, M. R. Boyd, Robin Pettit

Research output: Contribution to journalArticlepeer-review

16 Scopus citations


A new and more efficient synthesis of combretastatin A-3 (2a) was completed (8.4% overall yield) starting from methyl gallate and isovanillin with aldehyde 5 and phosphonium salt 8 as key intermediates. Conversion of combretastatin A-3 (2a) to a series of diphosphate prodrugs (10a-1) was readily achieved. Both the diphosphate sodium (10a) and potassium salts (10c) displayed aqueous solubility in excess of 220 mg/ml at room temperature and good cancer cell line inhibitory activity.

Original languageEnglish (US)
Pages (from-to)397-403
Number of pages7
JournalAnti-Cancer Drug Design
Issue number6
StatePublished - 2000


  • Cation salts
  • Combretastatin A-3
  • Diphosphate
  • Prodrugs

ASJC Scopus subject areas

  • Biochemistry
  • General Biochemistry, Genetics and Molecular Biology
  • Oncology
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry


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