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  • Title: Design, synthesis, and biological evaluation of substituted naphthalene imides and diimides as anticancer agent.
    Author: Tumiatti V, Milelli A, Minarini A, Micco M, Gasperi Campani A, Roncuzzi L, Baiocchi D, Marinello J, Capranico G, Zini M, Stefanelli C, Melchiorre C.
    Journal: J Med Chem; 2009 Dec 10; 52(23):7873-7. PubMed ID: 19954251.
    Abstract:
    Naphthalimmide (NI) and 1,4,5,8-naphthalentetracarboxylic diimide (NDI) derivatives were synthesized and evaluated for their antiproliferative activity. NDI derivatives 1-9 were more cytotoxic than the corresponding NI derivatives 10-18. The molecular mechanisms of 1 and 2 were investigated in comparison to mitonafide. They interacted with DNA, were not topoisomerase IIalpha poisons, triggered caspase activation, caused p53 protein accumulation, and down-regulated AKT survival. Furthermore, 1 and 2 caused a decrease of ERK1/2 and, unlike mitonafide, inhibited ERKs phosphorylation.
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