Advances in Prodrugs

Claudiu T. Supuran received his BSc and PhD in Chemistry from the Polytechnic Univesity of Bucharest (Romania), where he became an Assistant and then Associate Professor of Chemistry. In 1995, he moved to University of Florence, where he is Full Professor. His main research interest focused in medicinal chemistry, design of enzyme modulators especially in the carbonic anhydrase field, X-ray crystallography and molecular biology of metalloenzymes. He has published more than 1900 papers in these fields and his Hirsch index is 155, with > 105 700 citations. One of the compounds discovered in his laboratory (SLC-0111) is in Phase II clinical trials for the treatment of advanced metastatic solid tumors in Canada/USA, whereas a monoclonal antibody of which he is co-discoverer (6A10) is in preclinical evaluation and anti-tumor theragnotic agent. He is the editor-in-Chief of Journal of Enzyme Inhibition and Medicinal Chemistry and of Expert Opinion on Therapeutic Patents. Andrea Angeli obtained his MSc in Medicinal Chemistry and Technologies in 2014 and his PhD in Medicinal Chemistry in 2019 at the University of Florence (Italy). After he spent three years as Assistant researcher at the Centre of Advanced Research in Bionano conjugates and Biopolymers Department, “Petru Poni” Institute of Macromolecular Chemistry (Romania). From 2020 is visiting researcher to University of Florence. His research deals with several aspects of metalloenzymes, spanning from drug design, X-ray crystallography and synthesis of enzyme modulators. Damiano Tanini received his PhD degree in Chemistry in 2015 from the University of Florence working on the stereoselective synthesis of sulfur- and selenium-containing compounds. He carried out part of his doctoral research at the University of Bristol, working with Prof. V. K. Aggarwal. D. Tanini is currently a researcher in Organic Chemistry at the University of Florence. His research interests currently centre on organic synthesis, ranging from the development of sustainable methodologies towards bioactive molecules to the study of chalcogen-catalysed transformations and molecular chirality. D. Tanini serves as Editorial Board Member of several journals in chemical and biochemical area.

PART I: INTRODUCTION

1. PRODRUGS: GENERAL CONCEPTS, PRODRUG DESIGN IN MEDICINAL CHEMISTRY
Andrea Angeli, Claudiu T. Supuran and Damiano Tanini

PART II: ACTIVATION MECHANISMS AND RELATED FUNCTIONAL GROUPS
2. pH-SENSITIVE PRODRUGS
Emanuela Berrino
3. ENZYME-MEDIATED ACTIVATION OF PRODRUGS
Simone Carradori, Ilaria D'Agostino and Concettina La Motta
4. REACTIVE OXYGEN SPECIES-RESPONSIVE PRODRUGS
Jean-Yves Winum
5. PHOTOACTIVABLE PRODRUGS
Damiano Tanini
6. ANTIBODY DIRECTED ENZYME PRODRUG THERAPY (ADEPT)
Paolo Rovero, Andrea Di Santo and Anna Maria Papini
7. SELF-ASSEMBLING PRODRUGS
Mariana Pinteala V
8. PRODRUG-BASED NANOMEDICINES: A SUCCESSFUL RATIONALE TO DESIGN NOVEL AND EFFECTIVE DELIVERY STRATEGIES
Giulia Vanti
9. HYPOXIA-ACTIVATED PRODRUGS
Wagdy M. Eldehna

PART III: APPLICATION OF PRODRUGS IN THE TREATMENT OF DISEASES

10. ANTIVIRAL AND ANTIRETROVIRAL PRODRUGS
Claudiu T. Supuran and Luigi Pisano
11. PRODRUGS FOR CANCER THERAPY
Andrea Angeli
12. PRODRUGS FOR NEURODEGENERATIVE DISEASES
Paolo Guglielmi, Arianna Granese, Daniela Secci and Paola Chimenti
13. PRODRUGS IN CARDIOVASCULAR THERAPY
Laura Fumagalli and Angelica Artasensi
14. PRODRUGS FOR OCULAR DISEASES
Alessio Nocentini
15. ANTIBACTERIAL PRODRUGS
Raivis Žalubovskis
16. PRODRUGS AGAINST NEGLECTED DISEASES
ALANE BEATRIZ VERMELHO