Contacts:
Supervisors:
Prof. Valeria Di Bussolo, Dr. Lorenzo Biancalana
Title:
New glycoconjugation synthetic approaches for therapeutic and diagnostic applications
Abstract:
Glycoconjugation is currently a very investigated and applied procedure in the field of synthetic chemistry and clinical research and it has a key role in carbohydrate-based drugs and vaccines design. In the chemotherapy field it leads to molecules with therapeutic or diagnostic action mostly directed towards cancer cells, in consideration of an enhanced selectivity.
The aim of project is to merge metal complexes with a documented anticancer activity (ruthenium, osmium, iron and gold structures) with molecules such as glucose, glucose mimics or fructose, that can be recognized by GLUT’s and exploit their pathway. Moreover, in this project glycoconjugated-fluorescent probes will be developed as tumors diagnostic agents. These systems could allow to detect the presence of cancer cells, exploiting the fluorescence, in the visible or near IR region, of fluorophores such as coumarins.
Publications:
• F. D'Andrea, G. Vagelli, C. Granchi, L. Guazzelli, T. Tuccinardi, G. Poli, D. Iacopini, F. Minutolo, V. Di Bussolo, "Synthesis and Biological Evaluation of New Glycoconjugated LDH Inhibitors as Anticancer Agents", Molecules, 2019, 24(19), 3520. DOI:10.3390/molecules24193520
• G. Bononi, D. Iacopini, G. Cicio, S. Di Pietro, C. Granchi, V. Di Bussolo, F. Minutolo “Glycoconjugated metal complexes as cancer diagnostic and therapeutic agents”, ChemMedChem, 2020, 15, 1-36. DOI: 10.1002/cmdc.202000456
• D. Iacopini, A. Moscardini, F. Lessi, V. Di Bussolo, S. Di Pietro, G. Signore “Coumarin-based fluorescent biosensor with large linear range for ratiometric measurement of intracellular pH”, Bioorganic Chemistry, 2020, 105, 104372. DOI: 10.1016/j.bioorg.2020.104372
• S. Di Pietro, D. Iacopini, B. Storti, R. Nifosì, V. Di Bussolo, M. Pineschi, A. Moscardini, G. Signore and R. Bizzarri "New 1,3-Disubstituted Benzo[h]Isoquinoline Cyclen-Based Ligand Platform: Synthesis, Eu3+ Multiphoton Sensitization and Imaging Applications", Molecules, 2021, 26 (1), 58, DOI:10.3390/molecules26010058
• S. Di Pietro, V. Bordoni, D. Iacopini, S. Achilli, M. Pineschi, M. Thépaut, F. Fieschi, P. Crotti and V. Di Bussolo "New lipophilic glycomimetic DC-SIGN ligands: Stereoselective synthesis and SPR-based binding inhibition assays", Bioorganic Chemistry, 2021, 107, 104566, DOI:10.1016/j.bioorg.2020.104566
• S. Di Pietro, D. Iacopini, A. Moscardini, R. Bizzarri, M. Pineschi, V. Di Bussolo, G. Signore "New Coumarin Dipicolinate Europium Complexes with a Rich Chemical Speciation and Tunable Luminescence", Molecules, 2021, 26 (5), 1265, DOI:10.3390/molecules26051265
• D. Iacopini, G. Barbini, L. Favero, M. Pineschi, S. Di Pietro and V. Di Bussolo "Stereoselective Synthesis of New Pyran-Dioxane based Polycycles from Glycal Derived Vinyl Epoxide", Organic and Biomolecular Chemistry, 2021, DOI:10.1039/D1OB01541A
Oral communications at congress:
• “Stereoselective Synthesis of Glycoconjugates for Diagnostic Applications" D. Iacopini, S. Di Pietro, G. Signore, V. Di Bussolo, CFF 2021 - Chemistry for the Future- International Conference, Pisa - Dipartimento di Chimica e Chimica Industriale, June 30th-July 2nd 2021
• “Stereoselective Synthesis of Glycoconjugates for Diagnostic Applications" D. Iacopini, S. Di Pietro, G. Signore, V. Di Bussolo, Advanced School on Carbohydrate Chemistry (XVII CSCC-2021), Certosa di Pontignano (SI), 4th-7th July 2021
Poster communications at congress:
• "Stereoselective synthesis of new glycoconjugated Ruthenium(II)-Arene complexes as potential anticancer agents" D. Iacopini, L. Biancalana, S. Di Pietro, F. Marchetti, V. Di Bussolo, Eurocarb XX, Leiden (The Netherlands), June 30th - July 3rd 2019
• "Stereoselective synthesis of new glycoconjugated Ruthenium(II)-Arene complexes as potential anticancer agents" D. Iacopini, L. Biancalana, S. Di Pietro, F. Marchetti, V. Di Bussolo, CFF 2019 - Chemistry for the Future- International Conference, Pisa - Dipartimento di Chimica e Chimica Industriale, July 3rd - 5th 2019
