Quinazolinecarboline alkaloid evodiamine as scaffold for targeting topoisomerase i and sirtuins

Michael S. Christodoulou, Alessandro Sacchetti, Valentina Ronchetti, Stefania Caufin, Alessandra Silvani, Giordano Lesma, Gabriele Fontana, Fabrizio Minicone, Benedetta Riva, Micol Ventura, Maija Lahtela-Kakkonen, Elina Jarho, Valentina Zuco, Franco Zunino, Nadine Martinet, Federico Dapiaggi, Stefano Pieraccini, Maurizio Sironi, Lisa Dalla Via, Ornella Maria GiaDaniele Passarella

Research output: Contribution to journalArticle

Abstract

This paper reports the synthesis of a series of evodiamine derivatives. We assayed the ability to inhibit cell growth on three human tumour cell lines (H460, MCF-7 and HepG2) and we evaluated the capacity to interfere with the catalytic activity of topoisomerase I both by the relaxation assay and the occurrence of the cleavable complex. Moreover, whose effect on sirtuins 1, 2 and 3 was investigated. Finally, molecular docking analyses were performed in an attempt to rationalize the biological results.

Original languageEnglish
Pages (from-to)6920-6928
Number of pages9
JournalBioorganic and Medicinal Chemistry
Volume21
Issue number22
DOIs
Publication statusPublished - Nov 15 2013

Keywords

  • Evodiamine
  • Quinazolinecarboline alkaloids
  • Sirtuins
  • Topoisomerase I

ASJC Scopus subject areas

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

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  • Cite this

    Christodoulou, M. S., Sacchetti, A., Ronchetti, V., Caufin, S., Silvani, A., Lesma, G., Fontana, G., Minicone, F., Riva, B., Ventura, M., Lahtela-Kakkonen, M., Jarho, E., Zuco, V., Zunino, F., Martinet, N., Dapiaggi, F., Pieraccini, S., Sironi, M., Dalla Via, L., ... Passarella, D. (2013). Quinazolinecarboline alkaloid evodiamine as scaffold for targeting topoisomerase i and sirtuins. Bioorganic and Medicinal Chemistry, 21(22), 6920-6928. https://doi.org/10.1016/j.bmc.2013.09.030