Design, Synthesis, and Biological Evaluation of Substituted Naphthalene Imides and Diimides as Anticancer Agent
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- 作者：Vincenzo Tumiatti ; Andrea Milelli ; Anna Minarini ; Marialuisa Micco ; Anna Gasperi Campani ; Laura Roncuzzi ; Daniela Baiocchi ; Jessica Marinello ; Giovanni Capranico ; Maddalena Zini ; Claudio Stefanelli ; Ca
- 刊名：Journal of Medicinal Chemistry
- 出版年：2009
- 出版时间：December 10, 2009
- 年：2009
- 卷：52
- 期：23
- 页码：7873-7877
- 全文大小：751K
- 年卷期：v.52,no.23(December 10, 2009)
- ISSN：1520-4804
文摘
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 IIα 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.