Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4

Research output: Contribution to journalArticle

Abstract

Combretastatin A-4 disodiumphosphate (CA4P), a prodrug formulation of the natural product combretastatin A-4 (CA4), is currently in clinical investigation for the treatment of cancer. In vivo, CA4P is rapidly enzymatically converted to CA4, a potent inhibitor of tubulin polymerization (IC50 = 1-2 muM), and rapidly causes bloodflow shutdown in tumor tissues. A variety of alkyl and aryl di- and triesters of CA4P have been synthesized and evaluated as potential CA4 prodrugs and/or stable CAV analogues. (C) 2003 Elsevier Science Ltd. All rights reserved.

Details

Authors
  • MB Hadimani
  • Jianyi Hua
  • MD Jonklaas
  • RJ Kessler
  • Yezhou Sheng
  • A Olivares
  • RP Tanpure
  • A Weiser
  • JX Zhang
  • Klaus Edvardsen
  • RR Kane
  • KG Pinney
Organisations
Research areas and keywords

Subject classification (UKÄ) – MANDATORY

  • Immunology in the medical area
Original languageEnglish
Pages (from-to)1505-1508
JournalBioorganic & Medicinal Chemistry Letters
Volume13
Issue number9
Publication statusPublished - 2003
Publication categoryResearch
Peer-reviewedYes