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.
Medicinal Chemistry
Title:Synthesis and Evaluation of Cytotoxicity and Inhibitory Effect on Nitric Oxide Production by J774A.1 Macrophages of New Anthraquinone Derivatives
Volume: 9 Issue: 6
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
Affiliation:
Keywords: Mitoxantrone, anthraquinone derivatives, lipophilicity, cytotoxicity, nitric oxide production.
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.
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Alves S. Caio Cesar, Costa Da Cristiane F., Castro De Sandra B. R., Correa A. Tais, Santiago O. Gabriele, Diniz Renata, Ferreira Paula Ana and De Almeida V. Mauro, Synthesis and Evaluation of Cytotoxicity and Inhibitory Effect on Nitric Oxide Production by J774A.1 Macrophages of New Anthraquinone Derivatives, Medicinal Chemistry 2013; 9 (6) . https://dx.doi.org/10.2174/1573406411309060005
DOI https://dx.doi.org/10.2174/1573406411309060005 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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