Abstract
Increased attention has centered on exploiting hypoxia in tumors for targeting the design of selective antitumor agents. This review presents an update of the principal families of compounds under study and in clinical trials, such as Noxide derivatives, nitro compounds and quinone derivatives. Especially promising for bioreductive activation is the reduction of some moieties able to trigger a mechanism that releases cytotoxic antitumor drugs. The most remarkable redox-activated triggers are presented, N-oxide, nitro, azido, quinone, metal ions, 1,2-benzisoxazolyl and sulfoxide moieties.
Keywords: prodrug activation, antineoplastic drugs, Benzotriazine derivatives, QdNO derivatives, Redox-Activated Trigger
Medicinal Chemistry
Title: Development of Hypoxia Selective Cytotoxins for Cancer Treatment: An Update
Volume: 2 Issue: 3
Author(s): Hugo Cerecetto, Mercedes Gonzalez and Maria L. Lavaggi
Affiliation:
Keywords: prodrug activation, antineoplastic drugs, Benzotriazine derivatives, QdNO derivatives, Redox-Activated Trigger
Abstract: Increased attention has centered on exploiting hypoxia in tumors for targeting the design of selective antitumor agents. This review presents an update of the principal families of compounds under study and in clinical trials, such as Noxide derivatives, nitro compounds and quinone derivatives. Especially promising for bioreductive activation is the reduction of some moieties able to trigger a mechanism that releases cytotoxic antitumor drugs. The most remarkable redox-activated triggers are presented, N-oxide, nitro, azido, quinone, metal ions, 1,2-benzisoxazolyl and sulfoxide moieties.
Export Options
About this article
Cite this article as:
Cerecetto Hugo, Gonzalez Mercedes and Lavaggi L. Maria, Development of Hypoxia Selective Cytotoxins for Cancer Treatment: An Update, Medicinal Chemistry 2006; 2 (3) . https://dx.doi.org/10.2174/157340606776930808
DOI https://dx.doi.org/10.2174/157340606776930808 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
- 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
-
Preface
Central Nervous System Agents in Medicinal Chemistry Current and Future Neuropharmacological Options for the Treatment of Essential Tremor
Current Neuropharmacology Bottom-Up Proteomics
Current Analytical Chemistry Adjudin - A Male Contraceptive with Other Biological Activities
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Synthesis and Biological Evaluation of Quinazoline Derivatives as Potential Anticancer Agents (II)
Anti-Cancer Agents in Medicinal Chemistry Moving Beyond Tyrosine Hydroxylase to Define Dopaminergic Neurons for Use in Cell Replacement Therapies for Parkinson’s Disease
CNS & Neurological Disorders - Drug Targets Matrix Metalloproteinases: New Routes to the Use of MT1-MMP As A Therapeutic Target in Angiogenesis-Related Disease
Current Pharmaceutical Design Novel, Unifying Phagomimetic Mechanism of Vancomycin Therapeutic Action and Toxicity: Polyphenol, Electron Transfer and Reactive Oxygen Species
Anti-Infective Agents in Medicinal Chemistry Anti-Cancer Effect of Melatonin via Downregulation of Delta-like Ligand 4 in Estrogen-Responsive Breast Cancer Cells
Recent Patents on Anti-Cancer Drug Discovery Noradrenergic System in Down Syndrome and Alzheimer’s Disease A Target for Therapy
Current Alzheimer Research Role of Hexokinase and VDAC in Neurological Disorders
Current Molecular Pharmacology PET Studies of Brain Monoamine Transporters
Current Pharmaceutical Design The Framingham Brain Donation Program: Neuropathology Along the Cognitive Continuum
Current Alzheimer Research Recent Patents on Cardiovascular Stem Cells
Recent Patents on Cardiovascular Drug Discovery The Potential of Nasal Oxytocin Administration for Remediation of Autism Spectrum Disorders
CNS & Neurological Disorders - Drug Targets Medical Treatment of Critical Limb Ischemia: Current State and Future Directions
Current Vascular Pharmacology Isoniazid: Metabolic Aspects and Toxicological Correlates
Current Drug Metabolism Molecular Insight into the Crosstalk of UPS Components and Alzheimer’s Disease
Current Protein & Peptide Science Disease Outcome, Alexithymia and Depression are Differently Associated with Serum IL-18 Levels in Acute Stroke
Current Neurovascular Research Paeonol, a Powerful Natural Product with Broad Biological Spectra by Inhibiting Inflammatory Pathway
Current Traditional Medicine