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
-
Negative Regulation of TCR Signaling in Immunological Tolerance: Taming Good and Evil
Current Immunology Reviews (Discontinued) Editorial (Thematic Issue: Biologics in Autoimmune Diseases)
Current Pharmaceutical Biotechnology Evidence that Pregnancy Specific Glycoproteins Regulate T-Cell Function and Inflammatory Autoimmune Disease During Pregnancy
Current Drug Targets - Inflammation & Allergy DNA Vaccines: A Mini Review
Recent Patents on DNA & Gene Sequences Modulation of the Immune Response by the Cholera-like Enterotoxins
Current Topics in Medicinal Chemistry Pattern Recognition Receptors and Control of Innate Immunity: Role of Nucleic Acids
Current Pharmaceutical Biotechnology The Medical Functions of Probiotics and Their Role in Clinical Nutrition
Current Nutrition & Food Science siRNA Delivery Using Nanocarriers – An Efficient Tool for Gene Silencing
Current Gene Therapy Haematopoietic Stem Cell Gene Therapy to Treat Autoimmune Disease
Current Stem Cell Research & Therapy A New Approach to the Inflammatory/Autoimmune Diseases
Recent Patents on Anti-Infective Drug Discovery Scorpion Toxin Polyptides as Therapeutic Agents: An Overview
Protein & Peptide Letters Autoimmunity and Frontotemporal Dementia
Current Alzheimer Research Are B Cells a Potential Target for Therapeutic Intervention in the Classical T Cell-Mediated Autoimmune Disease Type 1 Diabetes?
Inflammation & Allergy - Drug Targets (Discontinued) Control of Autoimmune Diseases by the B7-CD28 Family Molecules
Current Pharmaceutical Design Immunotherapy for Multiple Sclerosis: Basic Insights for New Clinical Strategies
Current Neurovascular Research Thrombotic Microangiopathies: Towards a Pathophysiology-Based Classification
Cardiovascular & Hematological Disorders-Drug Targets Needle-free Gene Delivery Through the Skin: An Overview of Recent Strategies
Current Pharmaceutical Design Metabolic Changes in Autoimmune Diseases
Current Drug Discovery Technologies Synthetic Peptides: The Future of Patient Management in Systemic Rheumatic Diseases?
Current Medicinal Chemistry Viral Infection - A Cure for Type 1 Diabetes?
Current Medicinal Chemistry