Recent Developments in the Synthesis and Applications of Anticancer Amonafide Derivatives. A Mini Review

Author(s): Gary Gellerman

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 1 , 2016

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Graphical 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.

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

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Article Details

Year: 2016
Published on: 29 October, 2015
Page: [47 - 63]
Pages: 17
DOI: 10.2174/1570180812666150529205049

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