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.
Export Options
About this article
Cite this article as:
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Immunogenicity in Protein and Peptide Based-Therapeutics: An Overview
Current Protein & Peptide Science Novel Topical Nanocarriers for Treatment of Psoriasis: An Overview
Current Pharmaceutical Design Sjogrens Syndrome and Lymphoma Development
Current Immunology Reviews (Discontinued) Promises and Challenges of Adult Stem Cells in Cancer Therapy
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Oral Contraceptives and Autoimmune Diseases
Current Women`s Health Reviews Current and Potential Agents for the Treatment of Alopecia Areata
Current Pharmaceutical Design Tissue-specific Glucocorticoid Signaling May Determine the Resistance Against Glucocorticoids in Autoimmune Diseases
Current Medicinal Chemistry Involvement of IL-1R/TLR Signalling in Experimental Autoimmune Encephalomyelitis and Multiple Sclerosis
Current Molecular Medicine The Long and Winding Road: Searching for Non-MHC Psoriasis Susceptibility Loci
Current Genomics Modern Therapeutic Strategies for Autoimmune Diseases
Current Pharmaceutical Design Synthetic Peptides Derived from Ribosomal Proteins of Leishmania spp. in Mucocutaneous Leishmaniasis: Diagnostic Usefulness
Protein & Peptide Letters Mouse Models of Autoimmune Diseases: Immune Thrombocytopenia
Current Pharmaceutical Design Update on the Use of Biologics in Lupus
Current Pharmaceutical Biotechnology Cytokines as Novel Therapeutic Agents for Neuroinflammatory Disorders: A Role for Interferon-β in the Treatment of Multiple Sclerosis
Current Medicinal Chemistry - Central Nervous System Agents Involvement of Membrane Channels in Autoimmune Disorders
Current Pharmaceutical Design KIR Molecules: Recent Patents of Interest for the Diagnosis and Treatment of Several Autoimmune Diseases, Chronic Inflammation, and B-cell Malignancies
Recent Patents on DNA & Gene Sequences Update on ICOS: A Possible Target for Turning-Off Autoimmunity
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Acquired Hemophilia as Initial Presentation in a Patient with Systemic Lupus Erythematosus
Current Rheumatology Reviews Role of CD73 in Disease: Promising Prognostic Indicator and Therapeutic Target
Current Medicinal Chemistry Analogs of the Sea Anemone Potassium Channel Blocker ShK for the Treatment of Autoimmune Diseases
Inflammation & Allergy - Drug Targets (Discontinued)