TY - JOUR
T1 - Recent developments in the synthesis and applications of anticancer amonafide derivatives. A mini review
AU - Gellerman, Gary
N1 - Publisher Copyright:
© 2016 Bentham Science Publishers.
PY - 2016
Y1 - 2016
N2 - 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.
AB - 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.
KW - Addition-elimination
KW - Amonafide
KW - Anticancer
KW - Dual function
KW - Electrophilic aromatic substitution nucleophilic substitution
KW - One-pot synthesis
UR - http://www.scopus.com/inward/record.url?scp=84946592769&partnerID=8YFLogxK
U2 - 10.2174/1570180812666150529205049
DO - 10.2174/1570180812666150529205049
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AN - SCOPUS:84946592769
SN - 1570-1808
VL - 13
SP - 47
EP - 63
JO - Letters in Drug Design and Discovery
JF - Letters in Drug Design and Discovery
IS - 1
ER -