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Design, synthesis, and biological evaluation of substituted naphthalene imides and diimides as anticancer agent.
Tumiatti, Vincenzo; Milelli, Andrea; Minarini, Anna; Micco, Marialuisa; Gasperi Campani, Anna; Roncuzzi, Laura; Baiocchi, Daniela; Marinello, Jessica; Capranico, Giovanni; Zini, Maddalena; Stefanelli, Claudio; Melchiorre, Carlo.
Afiliação
  • Tumiatti V; Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy. vincenzo.tumiatti@unibo.it
J Med Chem ; 52(23): 7873-7, 2009 Dec 10.
Article em En | MEDLINE | ID: mdl-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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Imidas / Naftalenos / Antineoplásicos Idioma: En Ano de publicação: 2009 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Imidas / Naftalenos / Antineoplásicos Idioma: En Ano de publicação: 2009 Tipo de documento: Article