Abstract
Cisplatin is one of the chemotherapeutic agents used the most for testicular, ovarian and several other cancers. In order to overcome cisplatin resistance, other platinum (Pt) compounds have been developed and, in the last ten years, Pt-derivatives with reporting activity have also been synthesized. The first generation of reporting Pt-compounds was based on linking a fluorescent molecule (e.g. cyanine) to cisplatin, but more recent studies have focused on strategies to synthesize intrinsically fluorescent derivatives. Accordingly, bile acid Pt-compounds have shown fluorescence intensity that is stable at room temperature for a long time; this fluorescence is maintained after binding to oligonucleotides or DNA. Because of this, the binding mode of these compounds to DNA can be easily analyzed both by flow injection and fluorescence techniques, showing that although these compounds target the nuclei, they form adducts with the DNA that are different from those due to cisplatin. In line with this, these bile acid derivatives have shown increased cytotoxicity and ability to overcome resistance as compared to cisplatin in several cell lines. Moreover, in contrast to cisplatin, the activity of these compounds does not seem to be restricted to cycling cells but they also seem to kill resting cells. This review summarizes the information available on reporting Pt-compounds and focuses on these novel, intrinsically fluorescent bile acid Pt derivatives, their biochemical characteristics and biological activity.
Keywords: Intrinsically fluorescent, Pt(II) Complexes, Bile Acids, Flow Injection, Cytotoxic, Cisplatin analogues
Current Medicinal Chemistry
Title: Fluorescent Cisplatin Analogues and Cytotoxic Activity
Volume: 16 Issue: 32
Author(s): E. Rodriguez-Fernandez, J. L. Manzano, A. Alonso, M J. Almendral, M. Perez-Andres, A. Orfao and J. J. Criado
Affiliation:
Keywords: Intrinsically fluorescent, Pt(II) Complexes, Bile Acids, Flow Injection, Cytotoxic, Cisplatin analogues
Abstract: Cisplatin is one of the chemotherapeutic agents used the most for testicular, ovarian and several other cancers. In order to overcome cisplatin resistance, other platinum (Pt) compounds have been developed and, in the last ten years, Pt-derivatives with reporting activity have also been synthesized. The first generation of reporting Pt-compounds was based on linking a fluorescent molecule (e.g. cyanine) to cisplatin, but more recent studies have focused on strategies to synthesize intrinsically fluorescent derivatives. Accordingly, bile acid Pt-compounds have shown fluorescence intensity that is stable at room temperature for a long time; this fluorescence is maintained after binding to oligonucleotides or DNA. Because of this, the binding mode of these compounds to DNA can be easily analyzed both by flow injection and fluorescence techniques, showing that although these compounds target the nuclei, they form adducts with the DNA that are different from those due to cisplatin. In line with this, these bile acid derivatives have shown increased cytotoxicity and ability to overcome resistance as compared to cisplatin in several cell lines. Moreover, in contrast to cisplatin, the activity of these compounds does not seem to be restricted to cycling cells but they also seem to kill resting cells. This review summarizes the information available on reporting Pt-compounds and focuses on these novel, intrinsically fluorescent bile acid Pt derivatives, their biochemical characteristics and biological activity.
Export Options
About this article
Cite this article as:
Rodriguez-Fernandez E., Manzano L. J., Alonso A., Almendral J. M, Perez-Andres M., Orfao A. and Criado J. J., Fluorescent Cisplatin Analogues and Cytotoxic Activity, Current Medicinal Chemistry 2009; 16 (32) . https://dx.doi.org/10.2174/092986709789578169
DOI https://dx.doi.org/10.2174/092986709789578169 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
- Announcements
Related Articles
-
New Insights Toward Nanostructured Drug Delivery of Plant-Derived Polyphenol Compounds: Cancer Treatment and Gene Expression Profiles
Current Cancer Drug Targets Anti-Epidermal Growth Factor Receptor Antibodies in the Treatment of Metastatic Colorectal Cancer
Recent Patents on Anti-Cancer Drug Discovery Phosphatidylinositol 3-kinase Signaling as a Therapeutic Target for Cervical Cancer
Current Cancer Drug Targets Discovery, Structure and Biological Activities of the Cyclotides
Current Protein & Peptide Science Recent Patents on Live Bacteria and their Products as Potential Anticancer Agents
Recent Patents on Anti-Cancer Drug Discovery A Comprehensive Review on Combretastatin Analogues as Tubulin Binding Agents
Current Organic Chemistry γ-H2AX as a Therapeutic Target for Improving the Efficacy of Radiation Therapy
Current Cancer Drug Targets Carbon Nanotubes: An Emerging Drug Delivery Carrier in Cancer Therapeutics
Current Drug Delivery Universal Human Papillomavirus Vaccination and its Impact on the Southern Italian Region
Current Pharmaceutical Design Design, Synthesis, and Evaluation of Genistein Analogues as Anti-Cancer Agents
Anti-Cancer Agents in Medicinal Chemistry Radiopharmaceuticals for Oncology Drug Development: A Pharmaceutical Industry Perspective
Current Pharmaceutical Design The Type II Transmembrane Serine Protease, Matriptase-2: Possible Links to Cancer?
Anti-Cancer Agents in Medicinal Chemistry The Role of Targeted HIV Screening in the Emergency Department: A Scoping Review
Current HIV Research New Drug Design for Gene Therapy - Taking Advantage of Introns
Letters in Drug Design & Discovery Modulation of Signaling Enhances the Efficacy of the Combination of Satraplatin and Erlotinib
Current Drug Targets Editorial (Thematic Issue: Thyroid Cancer in Children and Adolescents)
Current Pediatric Reviews Role of Oxygen in Cancer: Looking Beyond Hypoxia
Anti-Cancer Agents in Medicinal Chemistry Vaccines and Other Immunological Approaches for Cancer Immunoprevention
Current Drug Targets Base Excision Repair, the Redox Environment and Therapeutic Implications
Current Molecular Pharmacology Quantum Dots in the Therapy: Current Trends and Perspectives
Mini-Reviews in Medicinal Chemistry