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Title: Synthesis and study of antiproliferative, antitopoisomerase II, DNA-intercalating and DNA-damaging activities of arylnaphthalimides
Authors: Quintana-Espinoza, Patricia
García-Luis, Jonay
Amesty, Ángel
Martín Rodríguez, Patricia 
Lorenzo-Castrillejo, Isabel
Ravelo, Angel G.
Fernández Pérez, Leandro Fco 
Machín, Félix
Estévez-Braun, Ana
UNESCO Clasification: 32 Ciencias médicas
2302 Bioquímica
Keywords: Topoisomerase-Ii
Homologous Recombination
Anticancer Agents
Amonafide, et al
Issue Date: 2013
Journal: Bioorganic and Medicinal Chemistry 
Abstract: A series of arylnaphthalimides were designed and synthesized to overcome the dose-limiting cytotoxicity of N-acetylated metabolites arising from amonafide, the prototypical antitumour naphthalimide whose biomedical properties have been related to its ability to intercalate the DNA and poison the enzyme Topoisomerase II. Thus, these arylnaphthalimides were first evaluated for their antiproliferative activity against two tumour cell lines and for their antitopoisomerase II in vitro activities, together with their ability to intercalate the DNA in vitro and also through docking modelization. Then, the well-known DNA damage response in Saccharomyces cerevisiae was employed to critically evaluate whether these novel compounds can damage the DNA in vivo. By performing all these assays we conclude that the 5-arylsubstituted naphthalimides not only keep but also improve amonafide's biological activities.
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2013.08.039
Source: Bioorganic & Medicinal Chemistry[ISSN 0968-0896],v. 21 (21), p. 6484-6495
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