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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Functionalization of Platinum Complexes for Biomedical Applications
Xiaoyong Wang1,2, Xiaohui Wang3,4, Zijian Guo3,2
1State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, State Key Laboratory of Analytical Chemistry for Life Science, Nanjing University , Nanjing 210023, P. R. China.
Abstract:
Platinum-based anticancer drugs are the mainstay of chemotherapy regimens in clinic. Nevertheless, the efficacy of platinum drugs is badly affected by serious systemic toxicities and drug resistance, and the pharmacokinetics of most platinum drugs is largely unknown. In recent years, a keen interest in functionalizing platinum complexes with bioactive molecules, targeting groups, photosensitizers, fluorophores, or nanomaterials has been sparked among chemical and biomedical researchers. The motivation for functionalization comes from some of the following demands: to improve the tumor selectivity or minimize the systemic toxicity of the drugs, to enhance the cellular accumulation of the drugs, to overcome the tumor resistance to the drugs, to visualize the drug molecules in vitro or in vivo, to achieve a synergistic anticancer effect between different therapeutic modalities, or to add extra functionality to the drugs. In this Account, we present different strategies being used for functionalizing platinum complexes, including conjugation with bisphosphonates, peptides, receptor-specific ligands, polymers, nanoparticles, magnetic resonance imaging contrast agents, metal chelators, or photosensitizers. Among them, bisphosphonates, peptides, and receptor-specific ligands are used for actively targeted drug delivery, polymers and nanoparticles are for passively targeted drug delivery, magnetic resonance imaging contrast agents are for theranostic purposes, metal chelators are for the treatment or prevention of Alzheimer's disease (AD), and photosensitizers are for photodynamic therapy of cancers. The rationales behind these designs are explained and justified at the molecular or cellular level, associating with the requirements for diagnosis, therapy, and visualization of biological processes. To illustrate the wide range of opportunities and challenges that are emerging in this realm, representative examples of targeted drug delivery systems, anticancer conjugates, anticancer theranostic agents, and anti-AD compounds relevant to functionalized platinum complexes are provided. All the examples exhibit new potential of platinum complexes for future applications in biomedical areas. The emphases of this Account are placed on the functionalization for targeted drug delivery and theranostic agents. In the end, a general assessment of various strategies has been made according to their major shortcomings and defects. The original information in this Account comes entirely from literature appearing since 2010.
Insights
Functionalizing platinum complexes enhances their anticancer efficacy by improving tumor targeting and reducing toxicity. This review explores strategies for targeted drug delivery and theranostic applications, showcasing new potential for platinum-based therapies.
Area of Science:
- * Medicinal Chemistry
- * Nanotechnology
- * Oncology
Background:
- * Platinum-based drugs are vital chemotherapy agents but face challenges like systemic toxicity and drug resistance.
- * Current platinum drugs have largely unknown pharmacokinetics, limiting their therapeutic optimization.
- * Functionalization of platinum complexes is a growing area of research to address these limitations.
Purpose of the Study:
- * To review strategies for functionalizing platinum complexes for improved anticancer therapy.
- * To highlight applications in targeted drug delivery, theranostics, and other biomedical areas.
- * To assess the opportunities and challenges in developing advanced platinum-based agents.
Main Methods:
- * Review of literature on functionalized platinum complexes published since 2010.
- * Categorization of functionalization strategies based on targeting mechanisms (active/passive) and applications.
- * Analysis of representative examples of targeted delivery systems, anticancer conjugates, theranostic agents, and anti-Alzheimer's compounds.
Main Results:
- * Functionalization strategies include conjugation with bisphosphonates, peptides, ligands, polymers, nanoparticles, imaging agents, and photosensitizers.
- * Active targeting utilizes bisphosphonates, peptides, and ligands; passive targeting uses polymers and nanoparticles.
- * Applications span targeted delivery, theranostics (imaging and therapy), and treatment of conditions like Alzheimer's disease.
Conclusions:
- * Functionalized platinum complexes offer significant potential for enhanced tumor selectivity, reduced systemic toxicity, and overcoming drug resistance.
- * Targeted drug delivery and theranostic applications represent key advancements in platinum-based chemotherapy.
- * Further research and assessment of functionalization strategies are needed to overcome existing shortcomings and realize the full potential of these agents.
