The research activity of the group is dedicated to the identification and characterization of new biologically active compounds. The inter-disciplinary approach is the driving force of the research activity which is focused on the design, synthesis and analysis of new focused compound libraries and on the preparation and characterization of chiral compounds. The group has prepared more than 1000 molecules (both natural and synthetic compounds) with drug-like properties. The biological investigations are carried out with several international collaborations.
Our laboratory is located at the Department of Drug Science of the University of Pavia
The registration for the 20th edition of the II level master in ‘Progettazione e Sviluppo dei Farmaci’ for the years 21-22 are OPEN!!!
- Identification of N,N-arylalkyl-picolinamide derivatives targeting the RNA-binding protein HuR, by combining biophysical fragment-screening and molecular hybridizationDella Volpe, S., Linciano, P., Listro, R., Tumminelli, E., Amadio, M., Bonomo, I., Elgaher, W.A.M., Adam, S., Hirsch, A.K.H., Boeckler, F.M., Vasile, F., Rossi, D., Collina, S. Bioorganic Chemistry, 116, 2021. DOI: 10.1016/j.bioorg.2021.105305 ABSTRACT. Hu proteins are members of the RNA-binding protein (RBP) family and play a pivotal role in the regulation of post-transcriptional processes. Through interaction with selected mRNAs,
- The registration for the 20th edition of the II level master in ‘Progettazione e Sviluppo dei Farmaci’ for the years 21-22 are OPEN!!!For more information, please visit the PSF Master Website
- Sigma-1 receptor agonists acting on aquaporin-mediated h2o2 permeability: New tools for counteracting oxidative stressPellavio, G., Rossino, G., Gastaldi, G., Rossi, D., Linciano, P., Collina, S., Laforenza, U. International Journal of Molecular Sciences, 22 (18), 2021. DOI: 10.3390/ijms22189790 ABSTRACT. Sigma1 Receptor (S1R) is involved in oxidative stress, since its activation is triggered by oxidative or endoplasmic reticulum stress. Since specific aquaporins (AQP), called peroxiporins, play a relevant role in controlling H2O2 permeability and ensure
- Identification of Compounds Targeting HuD. Another Brick in the Wall of Neurodegenerative Disease TreatmentAmbrosio, F.A., Coricello, A., Costa, G., Lupia, A., Micaelli, M., Marchesi, N., Sala, F., Pascale, A., Rossi, D., Vasile, F., Alcaro, S., Collina, S. Journal of Medicinal Chemistry, 64 (14), 2021. DOI: 10.1021/acs.jmedchem.1c00191 ABSTRACT. ELAV-like (ELAVL) RNA-binding proteins play a pivotal role in post-transcriptional processes, and their dysregulation is involved in several pathologies. This work was focused on HuD (ELAVL4),
- A composite nanosystem as a potential tool for the local treatment of glioblastoma: Chitosan‐coated solid lipid nanoparticles embedded in electrospun nanofibersVigani, B., Valentino, C., Sandri, G., Listro, R., Fagiani, F., Collina, S., Lanni, C., Bonferoni, M.C., Caramella, C.M., Rossi, S., Ferrari, F. Polymers, 13 (9), 2021. DOI: 10.3390/polym13091371 ABSTRACT. Glioblastoma multiforme (GBM) is one of the most prevalent and aggressive brain tumors for which there is currently no cure. A novel composite nanosystem (CN), consisting of chitosan-coated Solid Lipid Nanoparticles
- Gellan-based composite system as a potential tool for the treatment of nervous tissue injuries: Cross-linked electrospun nanofibers embedded in a RC-33-loaded freeze-dried matrixVigani, B., Valentino, C., Cavalloro, V., Catenacci, L., Sorrenti, M., Sandri, G., Bonferoni, M.C., Bozzi, C., Collina, S., Rossi, S., Ferrari, F. Pharmaceutics, 13 (2), 2021. DOI: 10.3390/pharmaceutics13020164 ABSTRACT. Injuries to the nervous system affect more than one billion people worldwide, and dramatically impact on the patient’s quality of life. The present work aimed to design and develop a gellan
- Microwave-assisted extraction and HPLC-UV-CD determination of (S)-usnic acid in cladonia foliaceaCavalloro, V., Marrubini, G., Stabile, R., Rossi, D., Linciano, P., Gheza, G., Assini, S., Martino, E., Collina, S. Molecules, 26 (2), 2021. DOI: 10.3390/molecules26020455 ABSTRACT. During the years, many usnic acid (UA) conjugates have been synthesized to obtain potent endowed with biological properties. Since (S)-UA is less abundant in nature than (R)-enantiomer, it is difficult to source, thus precluding a
- Enantiomeric Resolution and Absolute Configuration of a Chiral δ-Lactam, Useful Intermediate for the Synthesis of Bioactive CompoundsListro, R., Rossino, G., Della Volpe, S., Stabile, R., Boiocchi, M., Malavasi, L., Rossi, D., Collina, S. Molecules, 25(24), 2020. DOI: 10.3390/molecules25246023 ABSTRACT. During the past several years, the frequency of discovery of new molecular entities based on γ- or δ-lactam scaffolds has increased continuously. Most of them are characterized by the presence of at least one chiral center. Herein,
- Straightforward and direct access to β-seleno- amines and sulfonylamides via the controlled addition of phenylselenomethyllithium (LiCH2SePh) to iminesSenatore, R., Malik, M., Touqeer, S., Listro, R., Collina, S., Holzer, W., Pace, V. Tetrahedron, 76 (51), 2020. DOI: 10.1016/j.tet.2020.131220 ABSTRACT. The transfer of a α-methyl phenylseleno carbanion to variously functionalized N-aryl and N-sulfonyl imines is reported. The fast selenium-lithium exchange conducted on a diselenoacetal with n-BuLi enables the generation of the attacking homologative nucleophile under chemoselective conditions preserving concomitant potentially sensitive functionalities
- Setup and validation of a reliable docking protocol for the development of neuroprotective agents by targeting the Sigma-1 receptor (S1R)Rossino, G., Rui, M., Pozzetti, L., Schepmann, D., Wünsch, B., Zambieri, D, Pellavio, G., Laforenza, U., Rinaldi, S., Colombo, G., Morelli, L., Linciano, P., Rossi, D., Collina, S. Int. J. Mol. Sci. 2020. ABSTRACT. Sigma-1 receptor (S1R) is a promising molecular target for the development of novel effective therapies against neurodegenerative diseases. To speed up the discovery of new S1R modulators, herein we