Synthesis and cytotoxic activity of substituted Luotonin A derivatives

Sabrina Dallavalle, Lucio Merlini, Giovanni Luca Beretta, Stella Tinelli, Franco Zunino

Research output: Contribution to journalArticlepeer-review

Abstract

Luotonin A is a cytotoxic alkaloid that has been shown to inhibit topoisomerase I via stabilization of the binary complex topoisomerase-DNA in the same fashion as camptothecin. The synthesis and the cytotoxic activity on the lung carcinoma cell line H460 of a series of derivatives of Luotonin A is reported. The compounds inhibit topoisomerase I but show weak cytotoxic activity, thus confirming the peculiarity of ring E of camptothecin for antitumor activity.

Original languageEnglish
Pages (from-to)5757-5761
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number23
DOIs
Publication statusPublished - Dec 6 2004

Keywords

  • Antitumor agents
  • Cytotoxic alkaloid
  • Topoisomerase I

ASJC Scopus subject areas

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

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