Members Marco Radi
Marco Radi is Associate Professor of Medicinal Chemistry at the Department of Pharmacy of the University of Parma. He studied at the University of Siena (MSc cum Laude in Medicinal Chemistry, 2000; PhD in Medicinal Chemistry, 2004), doing his doctoral studies in solid-phase synthesis and antiviral drug-discovery with Maurizio Botta. He then did postdoctoral research at the University of Georgia (with David C.K. Chu; 2005-2006) where he pioneered the application of sub-zero microwave assisted technology for the synthesis of antiviral and anticancer nucleosides. He returned to the University of Siena as postdoctoral researcher (2006-2010) and then as untenured Assistant Professor (2010-2011). In December 2011 he moved to the University of Parma as permanent Assistant Professor at the School of Pharmacy, where he became Associate Professor in 2014.
Prof. Radi participated in different National (Programma per la Ricerca Regionale in Materia di Salute 2009; PRIN- 2007; PRIN-2008, PRIN-2010_2011, FIL-2012_2014) and International (CHAARM; ExCellENT-Hit; TRIoH; COST Angiokem, COST Glisten, Chiesi Foundation) multidisciplinary research projects. As PI or co-Investigator on these funded grants, he successfully administered the projects (e.g. recruitment, research planning, budget reports), collaborating with other international researchers and obtaining a few innovative results that led to several papers/patents: i) three different families of anti-HIV agents for drug-resistant forms (within TRIoH and CHAARM); ii) the first small molecule inhibitors of the human helicase DDX3 as broad-spectrum antivirals (within ExCellENT-Hit, PRIN-2008) Programma per la Ricerca Regionale in Materia di Salute 2009); iii) novel competitive and allosteric kinase inhibitors active on many different solid tumors (within COST Angiokem and PRIN-2007); iv) first-in-class Dengue Virus inhibitors (within FIL-2012_2014) and iv) broad spectrum antiviral agents (with the Chiesi Foundation grant).
He was also actively involved in the exploitation of the obtained research results by participating to the exclusive agreement between the University of Siena and Virostatics Srl for the licencing of the antitumor/antiviral compounds object of the patent application WO2009034547. He was involved in the exclusive agreement between the University of Siena and Centre National de la Recherche Scientifique (CNRS) for the licencing of the patent application WO2011073959. He was a co- author of the Business Plan “TKI Pharmaceutical”(based on the patent application WO2009034547) presented on 2006 at the scientific park Toscana Life Science. He was a co-author of the Business Plan “Lead Discovery Siena (LDS)” (based also on the patent application WO2009034547), winner of the 2009 edition of the Start Cup Toscana. He was a co-author and Proponent of the Business Plan “CoREX Pharm” (based on the patent application EP2388250) presented on 2012 at the scientific park Sardegna Ricerche. He was a co-author and Proponent of the Business Plan “AID-Discovery” (based on the patent application US 2012/0202814) presented on 2013 at the scientific park Sardegna Ricerche.
Prof. Radi is currently member of the Editorial Board of the Journal of Chemistry (since 2012), MC member of the COST Action CM1207 "GLISTEN” (since 2013) and Erasmus Delegate for the Department of Pharmacy (since 2012). He is member of the Department of Pharmacy and of the teacher board for the PhD programme "Drugs, Biomolecules and Health Products" at the University of Parma, where he supervise several undergraduates and PhD students in the field of medicinal chemistry. His present teaching activities are: i) Laboratory of drug analysis; ii) Database search for project planning. He is a peer reviewer for National (PRIN, FIRB, SIR) and International (IOFM, Horizon2020) research programs and referee for several medicinal chemistry and organic chemistry journals. Prof. Radi’s research activities are currently focused at the development of GPCRs modulators, enterovirus/rhinovirus inhibitors, kinase inhibitors, and Dengue virus inhibitors. His research interests are in the field of antiviral and anticancer drug discovery, with particular attention at the development of novel combinatorial methodologies to quickly produce highly functionalized chemical probes. He has authored more than 75 papers, book chapters and patent applications in these fields.
Selected publications:
- Radi, M., Tintori, C., Musumeci, F., Brullo, C., Zamperini, C., Dreassi, E., Fallacara, A.L., Vignaroli, G., Crespan, E., Zanoli, S., Laurenzana, I., Filippi, I., Maga, G., Schenone, S., Angelucci, A., Botta, M. Design, synthesis, and biological evaluation of pyrazolo[3,4-d]pyrimidines active in vivo on the Bcr-Abl T315I mutant (2013) Journal of Medicinal Chemistry, 56 (13), pp. 5382-5394. DOI: 0.1021/jm400233w
- Bellucci, L., Angeli, L., Tafi, A., Radi, M., Botta, M.
Unconventional plasticity of hiv-1 reverse transcriptase: How inhibitors could open a connection "gate" between allosteric and catalytic sites
(2013) Journal of Chemical Information and Modeling, 53 (12), pp. 3117-3122.
DOI: 10.1021/ci400414s - Radi, M., Evensen, L., Dreassi, E., Zamperini, C., Caporicci, M., Falchi, F., Musumeci, F., Schenone, S., Lorens, J.B., Botta, M. A combined targeted/phenotypic approach for the identification of new antiangiogenics agents active on a zebrafish model: From in silico screening to cyclodextrin formulation (2012) Bioorganic and Medicinal Chemistry Letters, 22 (17), pp. 5579-5583. DOI: 10.1016/j.bmcl.2012.07.014
- Radi, M., Falchi, F., Garbelli, A., Samuele, A., Bernardo, V., Paolucci, S., Baldanti, F., Schenone, S., Manetti, F., Maga, G., Botta, M. Discovery of the first small molecule inhibitor of human DDX3 specifically designed to target the RNA binding site: Towards the next generation HIV-1 inhibitors (2012) Bioorganic and Medicinal Chemistry Letters, 22 (5), pp. 2094-2098. DOI: 10.1016/j.bmcl.2011.12.135
- Freisz, S., Bec, G., Radi, M., Wolff, P., Crespan, E., Angeli, L., Dumas, P., Maga, G., Botta, M., Ennifar, E. Crystal structure of HIV-1 reverse transcriptase bound to a non-nucleoside inhibitor with a novel mechanism of action (2010) Angewandte Chemie - International Edition, 49 (10), pp. 1805-1808. DOI: 10.1002/anie.200905651
- Radi, M., Botta, L., Casaluce, G., Bernardini, M., Botta, M. Practical one-pot two-step protocol for the microwave-assisted synthesis of highly functionalized rhodanine derivatives (2010) Journal of Combinatorial Chemistry, 12 (1), pp. 200-205. DOI:10.1021/cc9001789
- Radi, M., Maga, G., Alongi, M., Angeli, L., Samuele, A., Zanoli, S., Bellucci, L., Tafi, A., Casaluce, G., Giorgi, G., Armand-Ugon, M., Gonzalez, E., Este, J.A., Baltzinger, M., Bec, G., Dumas, P., Ennifar, E., Botta, M. Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (5-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants (2009) Journal of Medicinal Chemistry, 52 (3), pp. 840-851. DOI:10.1021/jm801330n
- Maga, G., Falchi, F., Radi, M., Botta, L., Casaluce, G., Bernardini, M., Irannejad, H., Manetti, F., Garbelli, A., Samuele, A., Zanoli, S., Esté, J.A., Gonzalez, E., Zucca, E., Paolucci, S., Baldanti, F., DeRijck, J., Debyser, Z., Botta, M. Toward the Discovery of Novel Anti-HIV Drugs. Second-Generation Inhibitors of the Cellular ATPase DDX3 with Improved Anti-HIV Activity: Synthesis, Structure-Activity Relationship Analysis, Cytotoxicity Studies, and Target Validation (2011) ChemMedChem, 6 (8), pp. 1371-1389. DOI: 10.1002/cmdc.201100166
- Maga, G., Radi, M., Zanoli, S., Manetti, F., Cancio, R., Hübscher, U., Spadari, S., Falciani, C., Terrazas, M., Vilarrasa, J., Botta, M. Discovery of non-nucleoside inhibitors of HIV-1 reverse transcriptase competing with the nucleotide substrate (2007) Angewandte Chemie - International Edition, 46 (11), pp. 1810-1813. DOI: 110.1002/anie.200604165
