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.
Keywords: Amonafide, addition-elimination, electrophilic aromatic substitution nucleophilic substitution, one-pot synthesis,
dual function, anticancer.
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