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Synthesis and study of antiproliferative, antitopoisomerase II, DNA-intercalating and DNA-damaging activities of arylnaphthalimides

AutorMartín-Rodríguez, Patricia; Fernández-Pérez, Leandro; Estévez-Braun, Ana
Palabras claveTopoisomerase II
Antiproliferative activity
Saccharomyces cerevisiae
DNA damage
Fecha de publicación2013
CitaciónBioorganic and Medicinal Chemistry 21(21): 6484-6495 (2013)
ResumenA 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.
Descripciónet al.
Identificadoresdoi: 10.1016/j.bmc.2013.08.039
issn: 0968-0896
e-issn: 1464-3391
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