Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines

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

Research output: Contribution to journalArticle

21 Citations (Scopus)

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
Externally publishedYes

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Prodrugs
Cytotoxicity
Topoisomerase I Inhibitors
Cells
Neoplasms

Keywords

  • Antitumor
  • Dihydroindenoisoquinoline
  • Indenoisoquinoline
  • Prodrug
  • Topoisomerase I

ASJC Scopus subject areas

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

Cite this

Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines. / Xiao, Xiangshu; Miao, Ze Hong; Antony, Smitha; Pommier, Yves; Cushman, Mark.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 15, No. 11, 02.06.2005, p. 2795-2798.

Research output: Contribution to journalArticle

Xiao, Xiangshu ; Miao, Ze Hong ; Antony, Smitha ; Pommier, Yves ; Cushman, Mark. / Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines. In: Bioorganic and Medicinal Chemistry Letters. 2005 ; Vol. 15, No. 11. pp. 2795-2798.
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