Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines

Xiangshu Xiao, Ze Hong Miao, Smitha Antony, Yves Pommier, Mark Cushman

Research output: Contribution to journalArticle

23 Scopus citations

Abstract

Dihydroindenoisoquinolines are analogs of cytotoxic indenoisoquinoline topoisomerase I (Top1) inhibitors, exhibiting potent cytotoxicity but weak inhibitory activity toward Top1. Through COMPARE analysis, cytotoxicity studies in Top1-deficient cells, chemical synthesis and biological evaluation of methylated dihydroindenoisoquinoline 5, we demonstrated that dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines in cancer cells.

Original languageEnglish (US)
Pages (from-to)2795-2798
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number11
DOIs
StatePublished - Jun 2 2005

Keywords

  • Antitumor
  • Dihydroindenoisoquinoline
  • Indenoisoquinoline
  • Prodrug
  • Topoisomerase I

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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