New 7-aryl analogues of anthracyclines: Synthesis and cytotoxic activity of (+/-)-7-(3,4,5-trimethoxyphenyl)-7-deoxyidarubicinone

JC Acosta, E Caballero, DG Gravalos, M Medarde*, H Sahagun, RJ Stoodley, F Tome

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

The synthetic methodology for the preparation of 7-aryl-7-deoxyanthracyclinones, a new class of anthracycline analogues, is described. Readily available materials are easily transformed into the key intermediate ketone, that is converted into bent and planar tetracyclic compounds. Cytotoxic studies of the final and intermediate products reveal a moderate activity of bent products and a lack of activity of planar products, thus supporting a non-intercalating mechanism for their cytotoxic activity. (C) 1997 Elsevier Science Ltd.

Original languageEnglish
Pages (from-to)2955-2958
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume7
Issue number23
Publication statusPublished - 2 Dec 1997

Keywords

  • TUBULIN
  • RESOLUTION
  • COMBRETASTATIN
  • TRIMETREXATE
  • DNA
  • ANTITUMOR AGENT
  • NATURAL-PRODUCTS
  • PODOPHYLLOTOXIN
  • COLCHICINE
  • INHIBITION

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