1098129-38-4Relevant academic research and scientific papers
Synthesis and study of antiproliferative, antitopoisomerase II, DNA-intercalating and DNA-damaging activities of arylnaphthalimides
Quintana-Espinoza, Patricia,Garcia-Luis, Jonay,Amesty, Angel,Martin-Rodriguez, Patricia,Lorenzo-Castrillejo, Isabel,Ravelo, Angel G.,Fernandez-Perez, Leandro,Machin, Felix,Estevez-Braun, Ana
, p. 6484 - 6495 (2013)
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.
5-Non-amino aromatic substituted naphthalimides as potential antitumor agents: Synthesis via Suzuki reaction, antiproliferative activity, and DNA-binding behavior
Xie, Lijuan,Cui, Jingnan,Qian, Xuhong,Xu, Yufang,Liu, Jianwen,Xu, Ruian
, p. 961 - 967 (2011/03/17)
Amonafide is a naphthalimide derivative with antitumor activity and has failed to enter clinical phase III, because of its high-variable and unpredictable toxicity. In order to develop selective, efficient, and safe drugs, applying the 'nonfused' aromatic
