Design, synthesis, and biological evaluation of substituted naphthalene imides and diimides as anticancer agent∞

Vincenzo Tumiatti, Andrea Milelli, Anna Minarini, Marialuisa Micco, Anna Gasperi Campani, Laura Roncuzzi, Daniela Baiocchi, Jessica Marinello, Giovanni Capranico, Maddalena Zini, Claudio Stefanelli, Carlo Melchiorre

Research output: Contribution to journalArticlepeer-review

Abstract

Naphthalimmide (NI) and 1,4,5,8-naphthalentetracarboxylic diimide (NDI) derivatives were synthesized and evaluated for their antiproliferative activity. NDI derivatives 1-9 were more cytotoxic than the corresponding NI derivatives 10-18. The molecular mechanisms of 1 and 2 were investigated in comparison to mitonafide. They interacted with DNA, were not topoisomerase IIR poisons, triggered caspase activation, caused p53 protein accumulation, and down-regulated AKT survival. Furthermore, 1 and 2 caused a decrease of ERK1/2 and, unlike mitonafide, inhibited ERKs phosphorylation. ∞ Dedicated to Professor Fulvio Gualtieri on the occasion of his retirement.

Original languageEnglish
Pages (from-to)7873-7877
Number of pages5
JournalJournal of Medicinal Chemistry
Volume52
Issue number23
DOIs
Publication statusPublished - Dec 10 2009

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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