Bioinorganic Medicinal Chemistry

This book gives a comprehensive overview about medicinal inorganic chemistry. Topics like targeting strategies, mechanism of action, Pt-based antitumor drugs, radiopharmaceuticals are covered in detail and offer the reader an in-depth overview about this important topic. MEDICINAL INORGANIC CHEMISTRY: STATE OF THE ART, NEW TRENDS, AND A VISION OF THE FUTURE
Introduction
Antimicrobial Agents
Antiviral Agents
Systemic and Metabolic Diseases Including Inflammation
Metal Chelating Agents
Antiarthritic Drugs and Inflammation
Bipolar Disorder
Anticancer Agents
Small Molecule Delivery and Control
Diagnostic Agents
Veterinary Medicinal Inorganic Chemistry
Conclusions and Vision

TARGETING STRATEGIES FOR METAL-BASED THERAPEUTICS
Introduction
Physiological Targeting
Molecular Targeting
Immunological Targeting
Concluding Remarks

CURRENT STATUS AND MECHANISM OF ACTION OF PLATINUM-BASED ANTICANCER DRUGS
Introduction
Mechanism of Action of Cisplatin
Limitations of Current Platinum-Based Compounds: New Strategies
Novel Concepts in the Development of Platinum Antitumor Drugs
Concluding Remarks

NEW TRENDS AND FUTURE DEVELOPMENTS OF PLATINUM-BASED ANTITUMOR DRUGS
Introduction
Mechanisms of Action and Resistance
Monofunctional Platinum(II) Complexes
Trans-Platinum(II) Complexes
Multinuclear Platinum(II) C omplexes
Platinum(IV) Complexes
Delivery of Platinum Drugs
Concluding Remarks and Future Perspectives

RUTHENIUM AND OTHER NON-PLATINUM ANTICANCER COMPOUNDS
Introduction
Ruthenium Anticancer Compounds
From Gallium Nitrate to Oral Gallium Complexes
Titanium Anticancer Compounds
Ferrocene-Derived Anticancer Agents
The Main Group Organometallics Spirogermanium and Germanium-132
Arsenic in Cancer Chemotherapy
Overcoming the Resistance of Tumors to Anticancer Agents by Rare Earth Element Compounds
Conclusions

THE CHALLENGE OF ESTABLISHING RELIABLE SCREENING TESTS FOR SELECTING ANTICANCER METAL COMPOUNDS
Introduction
Tumor Cell Growth Inhibition and Cell Death Screening Assays
Metal-Based Anticancer Compounds and Gene Expression Microarray Technologies
Metal-Based Anticancer Compounds and the Proteomic Approach
Concluding Remarks

GOLD-BASED THERAPEUTIC AGENTS: A NEW PERSPECTIVE
Introduction
Biological Chemistry of Gold
Gold Antiarthritic Drugs
Gold Complexes as Anticancer Agents
Gold Complexes as Antiparasitic Agents
Concluding Remarks

MRI CONTRAST AGENTS: STATE OF THE ART AND NEW TRENDS
Introduction
T1 Agents
T2-Susceptibility Agents
CEST Agents
Concluding Remarks

METAL-BASED RADIOPHARMACEUTICALS
Introduction
Selected Examples: Therapeutic Radiopharmaceuticals
Diagnostic Metal-Based Radiopharmaceuticals
Perspectives and Conclusion

BORON AND GADOLINIUM IN THE NEUTRON CAPTURE THERAPY OF CANCER
Introduction
Boron Neutron Capture Therapy
Role of Medicinal Inorganic Chemistry in BNCT
Gadolinium Neutron Capture Therapy
Conclusions and Future Outlook

ESSENTIAL METAL RELATED METABOLIC DISORDERS
Introduction: What is Essentiality?
Iron Metabolic Diseases: Acquired and Genetic
Copper Metabolic Diseases
Zinc Metabolic Diseases
Diseases Related to Imbalances in Electrolytic Metabolism: P, the Alkali Metals, and the Alkaline Earths
Metabolism of Other Trace Elements
Conclusions

METAL COMPOUNDS AS ENZYME INHIBITORS
Introduction
Kinase Inhibitors
Proteasome Inhibitors
Carbonic Anhydrase Inhibitors (CAIs)
Cyclooxygenase Inhibitors
Acetylcholinesterase Inhibitors
Protein Phosphatase Inhibitors
Trypsin and Thrombin Inhibitors
Cysteine Protease Inhibitors and Glutathione Transferase Inhibitors
HIV-1 Reverse Transcriptase and Protease Inhibitors
Telomerase Inhibitors
Zinc Finger Protein Inhibitors
CXCR4 Inhibitors
Xanthine Oxidase Inhibitors
Miscellaneous Protein Inhibitors and Conclusions

BIOMEDICAL APPLICATIONS OF METAL-CONTAINING LUMINOPHORES
Introduction: Luminescence in Diagnostics and Imaging
Transition-Metal Containing Luminescent Agents
Lanthanide-Based Luminophores
Nanoparticle-Based Luninophores
Conclusions and Perspectives



Enzo Alessio was born in 1958, studied chemistry at the University of Trieste (Italy) and received his PhD from the University of Ferrara (Italy) in 1989. After a NATO-CNR postdoctoral fellowship with Luigi G. Marzilli at Emory University (Atlanta), he became fi rst Research Associate and then Associate Professor of Inorganic Chemistry at the University of Trieste, where he is now director of the PhD School in Chemistry. He is co-author of more than 150 publications and 10 patents in the fi elds of coordination chemistry, metal-based anticancer drugs, and metal-driven construction of supramolecular architectures, in particular multi-chromophore assemblies for photophysical applications. Medicinal Inorganic Chemistry represents a key area that comprises medical and biological inorganic chemistry. It is also currently an area of great excitement and achievements, where new approaches and ideas are thriving. The fi eld of metals in medicine represents approximately
a $3 billion/year industry. Pt-based cancer therapeutics are the major contributors to this bottom line, but relevant clinical success has been
achieved also in the area of Tc- and Gd-based imaging agents. It has become increasingly apparent, however, that metal-based pharmaceuticals can play a prominent role in areas outside of imaging and oncology, including those associated with the diagnosis and treatment of metabolic and genetic disorders, cardiovascular diseases, gene therapy, infl ammation, riperfusion injury, stroke, diabetes, ALS, malaria, and neurological diseases, to name but a few. This book is written by an international panel of experts in the fi eld and provides the reader with a ready reference to state-of-the-art Medicinal Inorganic Chemistry.

It is a must-have for Inorganic, Medicinal, and Bioinorganic Chemists, as well as Chemists working with Organometallics and in Industry.