TubInTrain
European Joint Doctorate on chemistry and biology of neurodegeneration, Horizon 2020 – Marie Skłodowska-Curie Innovative Training Networks
It is a plesure for us to introduce you the new European Joint Doctorate called TubInTrain. You can find more details on this ufficial Link.
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Quantitative Live Cell Imaging of a Tauopathy model enables the Identification of a Polypharmacological Drug Candidate that Restores Physiological Microtubule Interaction
Nature Communications, 2024
A live-cell imaging of a tauopathy model enables screening of compounds that modulate taumicrotubule interaction and allows identification of a promising polypharmacological drug candidate that simultaneously inhibits tau aggregation and reduces tau phosphorylation. Find out more at the link.
A Green Approach to Nucleophilic Aromatic Substitutions of Nicotinic Esters in Cyrene
European Journal of Organic Chemistry, 2024
Cyrene has been used as an eco-friendly alternative to environmentally harmful polar aprotic solvents in SNAr reactions. This innovative protocol enabled the facile synthesis of a wide library of novel nicotinic esters, valuable precursors of bioactive compounds. This methodology could also be extended to scale-up processes, microwave-assisted synthesis, and one-pot telescoping reactions, thus enhancing its applicability in various eco-friendly synthetic contexts. Find out more at the link.
Sustainable Synthesis of 1,2,3-Triazoles using Cyrene as a Biodegradable Solvent in Click Chemistry
ChemSusChem, 2025
The first successful synthesis of 1,2,3-triazoles using Cyrene as a biodegradable and non-toxic solvent in click chemistry has been developed. Find out more here.
Synthesis of α-fluorocinnamate derivatives as novel cathepsin S inhibitors with in vitro antiproliferative activity against pancreatic cancer cells
Bioorg. Med. Chem., 2025
We have designed and synthesized three new derivatives basing on an isosteric replacement (H–F) at the level of cinnamate moiety. These derivatives emerged as potent covalent inhibitors of CatS (1.8–2.6 µM) with 2F showing also weak inhibition activity against CatL (20 %) and CatB (29 %). In vitro assays of 2F against pancreatic cancer cell lines BXPC3 and CAPAN1 revealed significant antiproliferative activity, with IC50 = 5.79 µM and 20.75 µM, respectively.. To find out more details follow the page
Biochemical Modulation of D-Asp Metabolism in Brain
Discovery of new small molecules inhibitors of hDASPO for the treatment of disorders connected to deficiency of D-Asp levels in brain. hDASPO inhibitors increases D-Asp in neuronal cells and thereby activates NMDA receptor function.
hDASPO project covers several multidisciplinary aspects, such as structural biology, synthetic organic chemistry and pharmacology, in collaboration with prof. Marco Nardini (Unimi) and Loredano Pollegioni (Uninsubria).
Nicotinic Acid Derivatives As Novel Noncompetitive α-Amylase and α-Glucosidase Inhibitors for Type 2 Diabetes Treatment
ACS Medicinal Chemistry Letters, 2024
A library of novel nicotinic acid derivatives, focusing on the modification of position 6 of the pyridine ring with (thio)ether functionalities, was mostly produced through an innovative green synthetic approach (Cyrene-based) and evaluated for their α-amylase and α-glucosidase inhibitory activity. Find out more under the Link
First Total Synthesis of Caerulomycin K: a Case Study on Selective, Multiple C–H Functionalizations of Pyridines
RSC Advances, 2024
Caerulomycins, natural alkaloids with antimicrobial properties, have been previously synthesized starting with highly pre-functionalized building blocks or requiring many functional group manipulations. In this work, we report the first total synthesis of caerulomycin K, a diversely trifunctionalized pyridine readily assembled in three steps exploiting the recent advancements in the C–H activation of N-heterocycles. Find out more under the Link
Metal-Free, Selective Ortho-Deuteration of N-Heterocyclic Oxides
Adv. Synth. Cat., 2025
In this work, we present a metal-free, selective ortho-deuteration of N-heterocycles starting from their N-oxides, proceeding at room temperature in just 5 minutes. More about it at this link
Design, synthesis and in vitro validation of bivalent binders of SARS-CoV-2 spike protein: Obeticholic, betulinic and glycyrrhetinic acids as building blocks
Bioorg. Med. Chem., 2025
Bivalent compounds have been designed to simultaneously bind both pockets of the Spike protein, offering significant advantages over single molecules or the combination of the two natural products. In vitro cell assays using pseudotyped recombinant lentiviral particles with selected SARS-CoV-2 Spike proteins demonstrated that 1 and 2 exhibit enhanced activity in reducing viral entry into target cells compared to individual natural products. Check it out at this link
Self-Assembled Cannabigerol-Based Nanoparticles: Design, Synthesis, and Antiproliferative Activity
Pharmaceutics 2025, 17(5), 636; DOI: 10.3390/pharmaceutics17050636
Arianna Amenta, Giulia Nordio, Francesco Piazzola, Maria Luisa Di Paolo, Fabio Milani, Martina Giacomini,
Andrea Citarella,* Umberto Ciriello, Giuseppe Paladino, Sara Pellegrino, Federica Silvestri, Valerio Fasano,
Lisa Dalla Via* e Daniele Passarella
Access to Highly Functional and Polymerizable Carbonate-Drug Conjugates
ChemSusChem 2025, DOI: 10.1002/cssc.202500031
Wangyu Shi, Thirusangumurugan Senthamarai, Matteo Lanzi, Paolo Orlando, Rodrigo Nogués Martín, Arjan W. Kleij
Design, synthesis and in vitro validation of bivalent binders of SARS-CoV-2 spike protein: Obeticholic, betulinic and glycyrrhetinic acids as building blocks
Bioorganic & Medicinal Chemistry 2025, DOI: 10.1016/j.bmc.2025.118124
Martina Pedrini †, Luca Pozzi †, Francesca Sacchi, Andrea Citarella*, Valerio Fasano, Pierfausto Seneci, Stefano Pieraccini, Lorenzo Ruberto, Helena Perez Peña, Alfredo Garzino-Demo, Adriana Vitiello, Leonardo Sernicola, Alessandra Borsetti, Arianna Calistri, Cristina Parolin and Daniele Passarella*
Revisiting the Reduction of Vinpocetine
ChemistrySelect 2025, 10, e202406175, DOI: 10.1002/slct.202406175
Simone Borsoi, Luca Pozzi, Valerio Fasano, Andrea Citarella, Giovanni Macetti, Leonardo Lo Presti, Giuseppe Paladino, Umberto Ciriello and Daniele Passarella*
Mechanistic insights into the base-mediated deuteration of pyridyl phosphonium and ammonium salts
RSC Advances 2025, 15, 870 – 874, DOI: 10.1039/D4RA07557A
Arianna Montoli, Alessandro Dimasi, Miriana Guarnaccia, Andrea Citarella, Paolo Ronchi, Delia Blasi, Sergio Rossi, Daniele Passarella and Valerio Fasano*
Metal-free, Selective Ortho-Deuteration of N-heterocyclic Oxides
Advanced Synthesis and Catalysis 2025, e202401585,DOI: 10.1002/adsc.202401585
Arianna Montoli, Alessandro Dimasi, Andrea Citarella, Paolo Ronchi, Daniele Passarella and Valerio Fasano*
- The XLVIII edition of the “Attilio Corbella” International Summer School on Organic Synthesis (ISOS 2024) will take place in Gargnano (BS, Italy) on June 16-20, 2024.
https://corbellasummerschool.unimi.it/
- The XIV edition of the Italo-Spanish Symposium on Organic Chemistry (SISOC 2024) will take place in Turin on February 25-27, 2024.
