Synthesis and Evaluation of Cytotoxicity and Inhibitory Effect on Nitric Oxide Production by J774A.1 Macrophages of New Anthraquinone Derivatives

Author(s): Caio Cesar S. Alves, Cristiane F. Da Costa, Sandra B. R. De Castro, Tais A. Correa, Gabriele O. Santiago, Renata Diniz, Ana Paula Ferreira, Mauro V. De Almeida

Journal Name: Medicinal Chemistry

Volume 9 , Issue 6 , 2013

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Mitoxantrone is an anthracene-based anticancer agent whose efficacy in treating autoimmune diseases is believed to be due to cytotoxicity and inhibition of proliferation of cells. Several novel anthraquinone derivatives, analogs of mitoxantrone, were designed and synthesized. Lipophilic and functionalized mitoxantrone analogs were prepared by a simple methodology and the cytotoxicity and the inhibitory effect on nitric oxide release of these compounds were demonstrated in vitro on J774A.1 macrophages. Interestingly compounds 3, 4, 5, 6, 7, and 8 exhibited reduction in NO release (62.4%, 92.6%, 73.4%, 58.4%, 57.8% and 53.4%, respectively) in comparison to NG-n-methyl-arginine treated control, without cytotoxicity. In conclusion, anthraquinone derivatives were prepared in a good yield and showed promissory antiinflammatory properties.

Keywords: Mitoxantrone, anthraquinone derivatives, lipophilicity, cytotoxicity, nitric oxide production.

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Article Details

Year: 2013
Published on: 11 July, 2013
Page: [812 - 818]
Pages: 7
DOI: 10.2174/1573406411309060005
Price: $65

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