Publications of Last five years (since 2022)

1.         Te Liu, Romano Silvestri, et al. Aroyl diheterocyclic pyrrole (ARDHEP)@PLGA nanoparticles suppress human gastric cancer growth by modulating chromatin accessibility to activate the ZNF320-mediated cytokine-cytokine receptor pathway. J. Nanobiotechnology 2026, accepted (IF = 15.0).

2.         Marisol Zuniga, Alexander Herrmann, Matteo Rizzato, Adriana Fontes, Hans Zischka, Romano Silvestri, Andrea Brancale, Joachim J Bugert*, and Ruth Brack-Werner* Establishment of an in vitro human blood-brain barrier model for antiviral screening against neurotropic viruses. Fluids and Barriers of the CNS 2026, accept.

3.         Michela Puxeddu, Zeyu Cui, Claudia Colla, Simone Manetto, Alessia Ciogli, Petra Cuřínová, Marianna Bufano, Angelo Toto, Stefano Gianni, Giorgia Musto, Mariano Stornaiuolo, Enke Baldini, Salvatore Ulisse, Joanna Kopecka, Chiara Riganti, Chiara Bigogno, Giulio Dondio, Te Liu, Antonio Coluccia, La Regina, Romano Silvestri. (S,S)-5-Chloro-3-((3,5-dimethylphenyl)sulfonyl)-N-(1-oxo-1-((1-(pyridin-4-yl)ethyl)amino)propan-2-yl)-1H-indole-2-carboxamide, a New Dishevelled 1 and P-glycoprotein Dual Inhibitor as Anticancer Agent. J. Med. Chem. 2026, accept. https://doi.org/10.1021/acs.jmedchem.6c00706. PMCID# PMC13312410.

4.         Hongliang Shen; Zeyu Cui; Yilun Wu; Michela Puxeddu; Yanchen Lai; Ren Mo; Boyu Yang; Yinong Niu; Yichao Wen; Xiling Du; Romano Silvestri; Te Liu. Superparamagnetic iron oxide nanoparticle-driven 3-aroyl-1,4-diarylpyrrole nanocomposites (ARDAP@SPION-PEI) mediate renal cancer stem cell PANoptosis by regulating chromatin accessibility. Mol Biomed. 2026, 7, 70. doi: 10.1186/s43556-026-00470-z (IF = 10.1)

5.         Michela Puxeddu, Rosa Bordone, Claudia Colla, Gabriele Rotili, Antonio Coluccia, Pietro Sciò, Petra Cuřínová, Alessio Nocentini, Claudiu Supuran, Serena Filiberti, Marta Turati, Roberto Ronca, Joanna Kopecka, Chiara Riganti, Lucia Jimenez, Wolfgang Link, Chiara Bigogno, Giulio Dondio, Martina Barba, Gianluca Canettieri, Romano Silvestri, Giuseppe La Regina. 4-(5-Chloro-3-(3,4,5-trimethoxybenzoyl)-1H-indol-1-yl)benzenesulfonamide: A Novel Polypharmacology Agent to Target Carbonic Anhydrase IX and XII With Improved Selectivity, Wnt/β-Catenin Signaling Pathway and P-glycoprotein. ChemMedChem (special issue medicinal chemistry in Italy) 2026, 21, e202500996, https://doi.org/10.1002/cmdc.202500996.

6.         Roux H, Touret F, Coluccia A, Scio P, Bouzidi HS, di Giorgio C, Gattacceca F, Khoumeri O, Silvestri R, Vanelle P, Roche M. Design and synthesis of novel thioether analogs as promising antiviral agents: In vitro activity against enteroviruses of interest. Eur. J. Med. Chem. 2025, 288, 117395. doi: 10.1016/j.ejmech.2025.117395.

7.         Puxeddu, M.; Silvestri, R.; La Regina, G. Metabolism, a blossoming target for small molecule anti-cancer drugs. Molecules 2025, 30, 3457. https://doi.org/10.3390/molecules30173457.

8.         Masci D, Ling L, Yang L, Puxeddu M, Colla C, Coluccia A, Santelli M, Sciò P, Cuřínová P, Ansari MSZ, Naro C, Sette C, Jimenez L, Link W, Bigogno C, Dondio G, Hamel E, Liu T, Silvestri R, La Regina G. Ferroptosis Induction by a new pyrrole derivative in triple negative breast cancer and colorectal cancer. J Med Chem. 2025, 68, 17840-17858. doi: 10.1021/acs.jmedchem.5c01561. Correction: Masci D, Ling L, Yang L, Puxeddu M, Colla C, Coluccia A, Santelli M, Sciò P, Cuřínová P, Ansari MSZ, Naro C, Sette C, Jimenez L, Link W, Bigogno C, Dondio G, Hamel E, Liu T, Silvestri R. Ferroptosis Induction by a New Pyrrole Derivative in Triple Negative Breast Cancer and Colorectal Cancer. J Med Chem. 2025, 68, 17840-17858. doi: 10.1021/acs.jmedchem.5c01561. https://doi.org/10.1021/acs.jmedchem.6c00834

9.         Sciò P, Bufano M, Silvestri R, Coluccia A. Retrospective benchmarking and novel shape-pharmacophore based implementation of the MORLD Method for the autonomous optimization of 3-Aroyl-1,4-diarylpyrroles (ARDAP). J. Chem. Inf. Model. 2025, 65, 8819-8832. doi: 10.1021/acs.jcim.5c01276.

10.       Bonfanti, R. Silvestri, E. Novellino, G. C. Tenore, E. Schiano, F. Iannuzzo, M. Reverberi, L. Faino, M. Beccaccioli, F. Sivori, C. G. Rizzello, C. Mazzoni. Characterization of the microbial community of buffalo Mozzarella cheese whey and ricotta cheese exhausted whey. Investigation of the potential probiotics features of the subdominant autochthonous bacterial strains. Microorganisms 2025, 13, 1804. https://doi.org/10.3390/microorganisms13081804

11.       D. Masci, M. Puxeddu, C. Colla, A. Coluccia, M. Santelli, P. Sciò, E. Mariotto, G, Viola, E. Hamel, R. Lerose, C. Mazzoccoli, R. Silvestri, G La Regina. Microwave-assisted synthesis of tubulin assembly inhibitors as anticancer agents by aryl ring reversal and conjunctive approach. RSC Med. Chem. 2025, 16, 4845-4858.. doi: 10.1039/D5MD00406C.

12.       V. Pennacchietti, L. Pagano, M. Di Felice, J. Toso, M. Bufano, A. Coluccia, R. Silvestri, R. Capelli, C. Camilloni, F. Malagrinò, A, Toto, S. Gianni. Unveiling an unexpected redox regulation of the folding, function and inhibition in the PTB domain of FRS2. Int. J. Biol. Macromol. 2025, 309, Iss. Pt 2, doi: 10.1016/j.ijbiomac.2025.142478.

13.       M. Puxeddu, L. Ling, S. Ripa, M. D’Ambrosio, M. Nalli, A. Parisi, P. Sciò, A. Coluccia, A. Granese, M. Santelli, D. Masci, P. Cuřínová, C. Naro, C. Sette, A. Pastore, M. Stornaiuolo, C. Bigogno, G. Dondio, L. Di Magno, G. Canettieri, T. Liu, R. Silvestri, G. La Regina. Development of N-(4-(1H-imidazol-1-yl)phenyl)-4-chlorobenzenesulfonamide, a novel potent inhibitor of β-catenin with enhanced antitumor activity and metabolic stability. J. Med. Chem. 2024, 67, 20298−20314 doi: 10.1021/acs.jmedchem.4c01708.

14.       D. Masci, M. Puxeddu, R. Silvestri, G. La Regina. CBP and p300 targets for Wnt/b-catenin emerging anticancer Agents. Molecules 2024, 28, 4524.

15.       M. Puxeddu, M. Donalisio, J.J. Bugert, A. Corona, P. Cocomazzi, M. Milani, F. Hucke, I. Arduino, F. Esposito, P. Moretti, M.G. Ortore, M. Nalli, S. Manetto, G. Mazzoccanti, C. Bigogno, G. Dondio, P. Sciò, A. Coluccia, D. Lembo, E. Tramontano, R. Silvestri, E. Mastrangelo, G. La Regina. 4-(3-Phenylsulfonylindol-2-yl)-1-(pyridin-2-yl)piperazinyl-methanones as Potent Inhibitors of both SARS-CoV-2 and HCoV-OC43 Viruses. ACS Infectious Diseases 2024, 10, 3158-3175.  doi: 10.1021/acsinfecdis.4c00108

16.       H. Roux, F. Touret, A. Coluccia, O. Khoumeri, C. Majdi, P. Sciò, R. Silvestri, P.Vanelle, M. Roche. New potent EV-A71 antivirals targeting capsid. Eur. J. Med. Chem. 2024, 116658. https://doi.org/10.1016/j.ejmech.2024.116658.

17.       D. Masci, M. Puxeddu, R. Silvestri, G. La Regina. Metabolic rewiring in cancer: small molecule inhibitors in colorectal cancer therapy. Molecules 2024, 29, 2110. doi: https://doi.org/10.3390/molecules29092110.

18.       Ćurčić V, Olszewski M, Maciejewska N, Višnjevac A, Srdić-Rajić T, Dobričić V, García-Sosa AT, Kokanov SB, Araškov JB, Silvestri R, Schüle R, Jung M, Nikolić M, Filipović N.R. Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition. Arch Pharm (Weinheim) 2024, 357, e2300426. doi: 10.1002/ardp.202300426.

19.       D. Masci, C. Naro, M. Puxeddu, A. Urbani, C. Sette, G. La Regina, R. Silvestri. Recent advances in drug discovery for TNBC treatment. Molecules 2023, 28, 7513. Doi: https://doi.org/10.3390/molecules28227513.

20.       D. Masci, M. Puxeddu, L. Di Magno, M. D’Ambrosio, A. Parisi, M. Nalli, R. Bai, A. Coluccia, P. Sciò, V. Orlando, S. D’Angelo, S. Biagioni, A. Urbani, E. Hamel, A. Nocentini, S. Filiberti, M. Turati, R. Ronca, J. Kopecka, C. Riganti, C. Fionda, R. Bordone, G. Della Rocca, G. Canettieri, C. T. Supuran, R. Silvestri, G. La Regina. 4-(3-Phenyl-4-(3,4,5-trimethoxybenzoyl)-1H-pyrrol-1-yl)benzenesulfon-amide, a novel carbonic anhydrase and wnt/b-catenin signaling pathway dual targeting inhibitor with potent activity against multi-drug resistant cancer cells. J. Med. Chem. 2023, 66,14824-14842. Doi: 10.1021/acs.jmedchem.3c01424

21.       C. Mazzoccoli, F. Crispo, I. Laurenzana, M. Pietrafesa, L. Sisinni, R. Lerose, D. Telesca, M. R. Milella, T. Liu, J. Sebastiani, R. Silvestri, G. La Regina. Biological evaluation of (4-(4-Aminophenyl)-1-(4-fluorophenyl)-1H-pyrrol-3-yl)(3,4,5-trimethoxyphenyl)methanone as potential antineoplastic agent in 2D and 3D breast cancer models. Archiv der Pharmazie 2023, e2300354. https://doi.org/10.1002/ardp.202300354.

22.       Nalli M., Di Magno L., Wen Y., Liu X. D’Ambrosio, M., Puxeddu, M., Parisi A., Sebastiani, J., Sorato A., Ripa S., Di Pastena F., Capelli D, Montanari R., Masci D., Urbani A., Naro C., Sette C., Orlando V, D’Angelo S., Biagioni S., Bigogno C., Dondio G., Pastore A., Stornaiuolo M., Canettieri  G. Liu, T., Silvestri R., La Regina G. Novel N-(heterocyclylphenyl)benzensulfonamide sharing an unreported binding site with t-cell factor 4 at the β-catenin armadillo repeats domain as anticancer agent. ACS Pharmacol. Transl. Sci. 2023, 6, 1087-1103.doi:10.1021/acsptsci.3c00092. PMCID# PMC10353061.

23.       Marianna Bufano, Michela Puxeddu, Marianna Nalli, Giuseppe La Regina, Angelo Toto, Francesca Romana Liberati, Alessio Paone, Francesca Cutruzzolà, Domiziana Masci, Chiara Bigogno, Giulio Dondio, Romano Silvestri, Stefano Gianni, Antonio Coluccia.  Targeting the Grb2 cSH3 domain: design, synthesis and biological evaluation of the first series of modulators. Bioorganic Chemistry 2023, 138, 106607.

24.       Dvoracsko, Szabolcs; Dimmito, Marilisa Pia; Sebastiani, Jessica; La Regina, Giuseppe; Silvestri, Romano; Pieretti, Stefano; Tomboli, Csaba; Stefanucci, Azzurra; Mollica, Adriano. Rimonabant based compounds bearing hydrophobic amino acid derivatives as cannabinoid receptor subtype 1 ligand. ACS Med. Chem. Lett. 2023, 14, 479-486.

25.       K. R. Francisco, L. Monti, W. Wang, H. Park, L. J. Liu, D. Amarasinghe, M. Nalli, R. Silvestri, L. Guidi Magalhães, C. R. Caffreya. Structure-Activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei. Biorg Med. Chem. Lett. 2023, 81, 129123. https://doi.org/10.1016/j.bmcl.2023.129123

26.       R. Carnevale, V. Cammisotto, S. Bartimoccia, C. Nocella, M. Bufano, V. Castellani, L. Loffredo, S. Sciarretta, G. Frati, A. Coluccia, R. Silvestri, G. Ceccarelli, A. Oliva, M. Venditti, F. Pugliese, C. Mastroianni, O. Turriziani, M. Leopizzi, G. D’Amati, P. Pignatelli, F. Violi. Toll-Like Receptor 4-Dependent and Independent platelet-dependent thrombosis in SARS-CoV-2 Infection. Circulation Research 2023, 132, 290-305. doi: 10.1161/CIRCRESAHA.122.321541.

27.       F. R. Mammone, P. Rotundo, M. Puxeddu, R. Silvestri, R. Cirilli. Chemo- and enantio-selective reversed-phase HPLC analysis of rosuvastatin using a cellulose-based chiral stationary phase in gradient elution mode. Journal of Pharmaceutical and Biomedical Analysis 2023, 225, 115239.

28.       G. Giancotti, G. Nannetti, G. Padalino, M.Landini, N. Santos-Ferreira, J. Van Dycke, V. Naccarato, U. Patel, R. Silvestri, J. Neyts, R. Gozalbo-Rovira, J. Rodríguez-Díaz, J. Rocha-Pereira, A. Brancale, S. Ferla. Marcella Bassetto. Structural investigations on novel non-nucleoside inhibitors of human norovirus polymerase. Viruses 2022, 15, 74.

29.       F. R. Mammone, L. Zanitti, M. Puxeddu, G. La Regina, R. Silvestri, A. Borioni, R. Cirilli. A novel validated UHPLC method for the estimation of rosuvastatin and its complete impurity profile in tablet formulations. Molecules 2023, 28, 431.

30.       J. Sebastiani, M. Puxeddu, M. Nalli, R. Bai, L. Altieri, P. Rovella, E. Gaudio, D. Trisciuoglio, F. Spriano, P. Lavia, C. Fionda, D. Masci, A. Urbani, C. Bigogno, G. Dondio, E. Hamel, F. Bertoni, R. Silvestri, G. La Regina. RS6077 induces mitotic arrest and selectively activates cell death in human cancer cell lines and in a lymphoma tumor in vivo. Eur. J. Med. Chem. 2023, 246, 114997.

31.       M. Innocenti, R. Silvestri, M. Ceracchi, B. Silvestrini. Efficacy and safety of a novel food supplement in the treatment of functional dyspepsia: a pilot open study. Agro Food Industry Hi-Tech 2022 – ISSN 1722-6996

32.       M. Nalli, D. Masci, A. Urbani, G. La Regina, R. Silvestri. Emerging direct targeting β-catenin agents. Molecules 2022, 27, 7735-7747.

33.       M. Puxeddu, J. Wu, R.Bai, M. D’Ambrosio, M. Nalli, A. Coluccia, S. Manetto, A. Ciogli, D. Masci, A. Urbani, C. Fionda, S. Coni, R. Bordone, G. Canettieri, C. Bigogno, G. Dondio, E. Hamel, T. Liu, R. Silvestri, G. La Regina. Induction of ferroptosis in glioblastoma and ovarian cancers by a new pyrrole tubulin assembly inhibitor. J. Med. Chem. 2022, 65, 15805-15818 Doi: 10.1021/acs.jmedchem.2c01457. open access

34.       L. Jimenez, V. Mayoral-Varo, C. Amenábar, J. Ortega, M. Machuqueiro, R. Silvestri, A. Angeli, F. Carta, B. Ferreira, W. Link. Multiplexed cellular profiling using fluorescent fusion proteins identifies an inhibitor of CRM1-mediated nuclear export. Traffic 2022, 23, 587-599.

35.       L. Di Magno, A. Coluccia, Ma. Bufano, S. Ripa, G. La Regina, M. Nalli, G. Canettieri, R. Silvestri, L. Frati. Discovery of novel human lactate dehydrogenase inhibitors: structure-based virtual screening studies, in vitro and in vivo biological assessment. Eur. J. Med. Chem. 2022, 240, 114605. https://doi.org/10.1016/j.ejmech.2022.114605.

36.       M. Bufano, M. Laffranchi, S. Sozzani, D. Raimondo, R. Silvestri, A. Coluccia. Exploring CCRL2 Chemerin binding using Accelerated Molecular Dynamics. Proteins 2022, 1-7. Doi: 10.1002/prot.26348.

37.       A. Coluccia, M. Bufano, G. La Regina, M. Puxeddu, A. Toto, A. Paone, A. Bouzidi, G. Musto, N. Badolati, V. Orlando, S. Biagioni, Domiziana Masci, R. Cirilli, C. Cantatore, F. Cutruzzolà, S. Gianni, M. Stornaiuolo, R. Silvestri. (S)-5-Chloro-3-((3,5-dimethylphenyl)sulfonyl)-N-(1-oxo-1-((pyridin-4-ylmethyl)amino)propan-2-yl),1H-indole-2-carboxamide (RS4690) as a new Dishevelled 1 inhibitor. Cancers 2022, 14, 1358. https://doi.org/10.3390/cancers14051358.

38.       C. Cantatore, G. La Regina, R. Ferretti, R. Silvestri, R. Cirilli. Single-run chemo- and enantio-selective HPLC separation of tramadol and its principal metabolite, O-desmethyltramadol, using a chlorinated immobilized amylose-based chiral stationary phase under multimodal elution conditions. Sep. Sci. Plus 2022, 5, 99-104. https://doi.org/10.1002/sscp.202200009. IF 2020 = 3.645.

39.       C. Passirani, A. Vessières, G. La Regina, W. Link, R. Silvestri. Modulating undruggable targets to overcome cancer therapy resistance. Drug Resistance Updates 2022, 60, 100788. https://doi.org/10.1016/j.drup.2021.100788. IF = 18.50