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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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 and Mauro V. De Almeida

Volume 9, Issue 6, 2013

Page: [812 - 818] Pages: 7

DOI: 10.2174/1573406411309060005

Price: $65

Abstract

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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