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Department of Pharmacy and Biotechnology - FABIT

Medicinal Chemistry - Natural products’ inspired molecules. Coordinator: Bisi

Design and synthesis of bioactive small molecules, as potential drug candidates, based on oxa- and azaheterocyclic scaffolds, related to different classes of natural compounds (such as flavonoids and coumarins)

Areas: Drug discovery and development

Research themes

Research involves the design and synthesis of bioactive small molecules as potential drug candidates. Scaffolds are mainly oxa- and azaheterocycles, related to different classes of natural products. These molecules can be considered as privileged structures and carriers that, when differently functionalized with appropriate pharmacophore moieties, can tailor the activity towards one or more targets involved in complex pathologies.

Main research themes are related to the development of molecules able to modulate the activities of:

  • targets involved in the development of neurodegenerative disorders such as cholinesterases, kinases, FAAH and cannabinoids receptors, trascription factor Nrf-2
  • cytochromes P450 involved in the biosynthesis of estrogens and of estrogen receptors as antitumor agents
  • enzymes involved in tumor progression and multiple drug resistance (MDR)
  • key enzymes for the development of tropical parasitic diseases such as malaria, leishmanial infections and trypanosomiasis

Lab members

Alessandra Bisi - Associate Professor (scrivi) 

Silvia Gobbi - Associate Professor (scrivi)

Federica Belluti - Associate Professor (scrivi)

Angela Rampa -  Alma Mater Professor (scrivi)

Rebecca Orioli - PhD Student

Elena Roggiolani - Scholarship Holder

Internship projects

Internship for the preparation of a degree thesis has a duration of more or less 8 months and involves the synthesis, purification and structural characterization of bioactive small molecules. The student takes part in one of the ongoing projects of the research group, in particular neurodegeneration, tumor or parasitic neglected diseases. 4/6 positions are available per year.

 

Main publications

Caciolla, J.; Martini, S.; Spinello, A.; Pavlin, M.; Turrini, E.; Simonelli, F.; Belluti, F.; Rampa, A.; Bisi, A.; Fimognari, C.; Zaffaroni, N.; Gobbi, S.; Magistrato, A. Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer. Eur. J. Med. Chem. (2021), 224, 113733  doi: 10.1016/j.ejmech.2021.113733.

Caciolla, J.; Picone, G.; Farruggia, G.; Valenti, D.; Rampa, A.; Malucelli, E.; Belluti, F.; Trezza, A.; Spiga, O.; Iotti, S.;  Gobbi, S.; Cappadone, C.; Bisi, A. Multifaceted activity of polyciclic MDR revertant agents in drug-resistant leukemic cells: Role of the spacer. Bioorg Chem. (2021) 106, 104460. doi: 10.1016/j.bioorg.2020.104460.

Di Martino, R.M.C.; Pruccoli, L.; Bisi, A.; Gobbi, S.; Rampa, A.;  Martinez, A.; Pérez, C.; Martinez-Gonzalez, L.; Paglione, M.; Di Schiavi, E.; Seghetti, F.; Tarozzi, A.; Belluti, F. Novel Curcumin-Diethyl Fumarate Hybrid as a Dualistic GSK-3β Inhibitor/Nrf2 Inducer for the Treatment of Parkinson's Disease. ACS Chem Neurosci. (2020,  11, 2728-2740. doi: 10.1021/acschemneuro.0c00363.

Bonvicini, F.; Manet, I.; Belluti, F.; Gobbi, S.; Rampa, A.; Gentilomi, G.A.; Bisi, A. Targeting the Bacterial Membrane with a New Polycyclic Privileged Structure: A Powerful Tool To Face Staphylococcus aureus Infections. ACS Infect Dis. (2019), 5, 1524-1534. doi: 10.1021/acsinfecdis.9b00072.

Ortalli, M.; Ilari, A.; Colotti, G.; De Ionna, I.; Battista, T.; Bisi, A.; Gobbi, S.; Rampa, A.; Di Martino, R. M. C.; Gentilomi, G.A.; Varani, S.; Belluti, F. Identification of chalcone-based antileishmanial agents targeting trypanothione reductase. Eur. J. Med. Chem. (2018), 152, 527-541. doi: 10.1016/j.ejmech.2018.04.057

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