Recent developments in the synthesis and applications of anticancer amonafide derivatives. A mini review

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Abstract

Among anticancer DNA-intercalating agents, medicinally important 1,8-naphthalimide derivatives represent an important class of bioleads possessed substantial cytotoxic activity toward a variety of murine and human cancercells. Amonafide, as the representative of this family, plays an important role due to its potent antitumor properties. Amonafide is a topoisomerase II (Topo II) inhibitor and DNA intercalator that induces apoptosis by inhibiting the binding of Topo II to the double strand DNA and also preserves anticancer activity even in the presence of multi-drug resistance (MDR), a main contributor to adjuvant therapeutic failure. In this review are summarized recent developments in the synthesis of amonafide derivatives and their bioactivity. In addition, the effect of structural characteristicsof such agents on structure activity relationship (SAR) will be also discussed.

Original languageEnglish
Pages (from-to)47-63
Number of pages17
JournalLetters in Drug Design and Discovery
Volume13
Issue number1
DOIs
StatePublished - 2016

Keywords

  • Addition-elimination
  • Amonafide
  • Anticancer
  • Dual function
  • Electrophilic aromatic substitution nucleophilic substitution
  • One-pot synthesis

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