title: Design, synthesis, and biological evaluation of substituted naphthalene imides and diimides as anticancer agent.
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.
authors: Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy. vincenzo.tumiatti@unibo.it
authors: Vincenzo
authors: V
authors: Tumiatti
authors: Andrea
authors: A
authors: Milelli
authors: Anna
authors: A
authors: Minarini
authors: Marialuisa
authors: M
authors: Micco
authors: Anna
authors: A
authors: Gasperi Campani
authors: Laura
authors: L
authors: Roncuzzi
authors: Daniela
authors: D
authors: Baiocchi
authors: Jessica
authors: J
authors: Marinello
authors: Giovanni
authors: G
authors: Capranico
authors: Maddalena
authors: M
authors: Zini
authors: Claudio
authors: C
authors: Stefanelli
authors: Carlo
authors: C
authors: Melchiorre
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004247:DNA / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D007094:Imides / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D009281:Naphthalenes / Q000737:chemistry*; D059003:Topoisomerase Inhibitors
chemical_list: D000970:Antineoplastic Agents; D007094:Imides; D009281:Naphthalenes; D059003:Topoisomerase Inhibitors; C031721:naphthalene; D004247:DNA