Prof. Romano Silvestri is Full Professor of Medicinal Chemistry at the Sapienza University of Rome, Italy. He graduated cum laude from Sapienza University and completed his PhD studies in Pharmaceutical Sciences by the same University. Since being recruited to the Department of Pharmaceutical Studies, he became Assistant Professor (1991-1998) and Associate Professor (1998-2010). In 2008 he moved to Department of Drug Chemistry and Technologies, and in 2010 became Full Professor. In 2015 was visting professor at Emory University, Department of Chemistry, Atlanta, USA (prof. Dennis Liotta), and in 2016 at King’s College, London (UK).
EDUCATION
983 B.S. cum laude in Pharmacy
1989 Ph.D., Pharmaceutical Sciences
1991-1998 Assistant Professor
1998-2010 Associate Professor
2010- Full Professor
2012- Director of School in Hospital Pharmacy
RESEARCH INTERESTS
The research projects are mainly focused on the drug design and synthesis of new biologically active chemical entities in the areas of antitumor, antiviral or SNC drugs. The drug design is based on molecular models performed by the internal computaional unit. New procedures for the microwave-assiste
FUTURE PROJECTS
Targeting beta-catenin and Dishevelled protein as a synergistic strategy against colorectal cancer
Applications Invited
219
Scopus Publications
Scopus Publications
Superparamagnetic iron oxide nanoparticle-driven 3-aroyl-1,4-diarylpyrrole nanocomposites (ARDAP@SPION-PEI) mediate renal cancer cell PANoptosis by regulating chromatin accessibility Hongliang Shen, Zeyu Cui, Yilun Wu, Michela Puxeddu, Yanchen Lai, Ren Mo, Boyu Yang, Yinong Niu, Yichao Wen, Xiling Du, Romano Silvestri, Te Liu Molecular Biomedicine, 2026 The renal cancer stem cells (RCSCs) have highly proliferation, resistance to radiotherapy and chemotherapy, and enhanced invasive and tumorigenic capacities characteristics. 3-Aroyl-1,4-diarylpyrrole (ARDAP) is a potent microtubule inhibitor developed by our team; however, its specific killing effects on RCSCs remain unknown. Furthermore, clinical application of ARDAP is restricted by shortcomings such as poor water solubility and low utilization rates. Here, we developed polyethylenimine-coated superparamagnetic iron oxide nanoparticles loaded with ARDAP (ARDAP@SPION-PEI) to overcome these barriers and evaluated their efficacy in mouse RCSCs (mRCSCs) and zebrafish. In vitro and in vivo experiments demonstrated that ARDAP@SPION-PEI significantly inhibited mRCSCs proliferation, migration, and tumorigenicity while suppressing angiogenesis in zebrafish. ARDAP@SPION-PEI treatment significantly upregulated the expression of key PANoptosis pathway genes. Assay for transposase-accessible chromatin using sequencing revealed widespread chromatin accessibility alterations, with prominent enrichment of the transcription factor zinc finger protein 148 (ZFP148). Luciferase reporter assays demonstrated that ZFP148 directly bound to and activated promoters of key PANoptosis-related genes, including receptor-interacting serine/threonine kinase 3 ( Ripk3 ), gasdermin D ( Gsdmd ), IL-1β ( Il1b ), and caspase-1 ( Casp1 ). Chromatin immunoprecipitation–polymerase chain reaction further showed significantly enhanced promoter occupancy at the histone H3 lysine 4 trimethylation site following treatment, indicating transcriptionally active chromatin states. Silencing ZFP148 attenuated gene activation and reduced cell death induction. In conclusion, ARDAP@SPION-PEI induces mRCSC PANoptosis by remodeling chromatin structure to promote ZNF148-mediated transcription, offering a promising epigenetic-based nanotherapeutic strategy for renal cancer.
Correction to “Ferroptosis Induction by a New Pyrrole Derivative in Triple Negative Breast Cancer and Colorectal Cancer” Domiziana Masci, Lele Ling, Lian Yang, Michela Puxeddu, Claudia Colla, Marianna Nalli, Antonio Coluccia, Martina Santelli, Pietro Sciò, Petra Cuřínová, Mohammad Salik Zeya Ansari, Chiara Naro, Claudio Sette, Lucia Jimenez, Wolfgang Link, Chiara Bigogno, Giulio Dondio, Ernest Hamel, Te Liu, Romano Silvestri, Giuseppe La Regina Journal of Medicinal Chemistry, 2026
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 Michela Puxeddu, Rosa Bordone, Claudia Colla, Gabriele Rotili, Antonio Coluccia, et al. Chemmedchem, 2026 We synthesized novel pyrrole (5-11) and indole (12-16) derivatives based on a polypharmacology approach aimed to obtain inhibitors of human carbonic anhydrase (hCA) with improved selectivity toward the IX and XII isoforms, Wnt/β-catenin pathway, and P-glycoprotein (P-gp). Inspection of the binding sites of the hCA I, II, IX, and XII isoforms highlighted small but significant differences of cavity volumes that guided the introduction of small substituents at Position 4 of the 3-phenyl ring of the pyrrole and at Position 5 of the indole. Compound 15 exhibited potent and selective inhibition of both hCA IX and XII isoforms compared to the parent compound. It inhibited the Wnt/β-catenin pathway abrogating the association of β-catenin with TCF-4 and the multidrug-resistant P-gp-expressing cancer cells. Compound 15 showed strong inhibition of viability of SW620, SW480, and HCT116 CRC and TNBC cell lines, restored the sensitivity to doxorubicin (DOX) in HT29/DX P-gp-overexpressing cells, and showed medium metabolic stability in both human and mouse microsomes and acceptable predicted oral bioavailability. Compound 15 is a robust lead compound for the development of new antitumor agents based on the polypharmacology approach.
Metabolism, a Blossoming Target for Small-Molecule Anticancer Drugs Michela Puxeddu, Romano Silvestri, Giuseppe La Regina Molecules, 2025 Reprogramming is recognized as a promising target in cancer therapy. It is well known that the altered metabolism in cancer cells, in particular malignancies, are characterized by increased aerobic glycolysis (Warburg effect) which promotes rapid proliferation. The effort to design compounds able to modulate these hallmarks of cancer are gaining increasing attention in drug discovery. In this context, the present review explores recent progress in the development of small molecule inhibitors of key metabolic pathways, such as glycolysis, glutamine metabolism and fatty acid synthesis. In particular, different mechanisms of action of these compounds are analyzed, which can target distinct enzymes, including LDH, HK2, PKM2, GLS and FASN. The findings underscore the relevance of metabolism-based strategies in developing next-generation anticancer agents with potential for improved efficacy and reduced systemic toxicity.
Ferroptosis Induction by a New Pyrrole Derivative in Triple Negative Breast Cancer and Colorectal Cancer Domiziana Masci, Lele Ling, Lian Yang, Michela Puxeddu, Claudia Colla, Antonio Coluccia, Martina Santelli, Pietro Sciò, Petra Cuřínová, Mohammad Salik Zeya Ansari, Chiara Naro, Claudio Sette, Lucia Jimenez, Wolfgang Link, Chiara Bigogno, Giulio Dondio, Ernest Hamel, Te Liu, Romano Silvestri, Giuseppe La Regina Journal of Medicinal Chemistry, 2025 Ferroptosis-inducing agents are an emerging class of nonapoptotic, iron-dependent compounds for anticancer chemotherapy. We describe the synthesis of new aroyl diheterocyclyl pyrrole derivatives 2–21 . Compound 12 exhibited the most potent in vitro anticancer activity against breast cancer (BC), triple-negative breast cancer (TNBC), and colorectal cancer (CRC) cell lines, as well as significant efficacy in an HCT116 CRC xenograft model. Compound 12 showed typical hallmarks of ferroptosis in HCT116 cells from tumor tissues both in immunofluorescence and a qPCR gene assay and in the expression of ferroptosis inhibited proteins. Compound 12 significantly lowered GSH, NADP +, and NADPH levels. Furthermore, lactoperoxidase, malondialdehyde, and Fe(II) levels significantly increased in 12 -treated tissues, whereas superoxide dismutase concentrations decreased. Taken together, these results indicate that the antitumor activity of compound 12 was caused by the strong induction of ferroptosis. Given its high activity, compound 12 represents a promising therapeutic candidate for TNBC and CRC.
Retrospective Benchmarking and Novel Shape-Pharmacophore Based Implementation of the MORLD Method for the Autonomous Optimization of 3-Aroyl-1,4-diarylpyrroles (ARDAP) Pietro Sciò, Marianna Bufano, Romano Silvestri, Antonio Coluccia Journal of Chemical Information and Modeling, 2025 The use of artificial intelligence (AI) is increasingly integral to the drug-discovery process, and among AI-driven methodologies, deep generative models stand out as one of the most promising approaches for hit identification and optimization. Here, we report a retrospective benchmarking analysis of a series of tubulin inhibitors, 3-aroyl-1,4-diarylpyrroles (ARDAP), using the deep-generative algorithm Molecule Optimization by Reinforcement Learning and Docking (MORLD) in combination with five docking software (QuickVina 2, AutoDock-GPU, PLANTS, GOLD, and Glide). Our results indicate that the performance of the MORLD/docking workflow is highly dependent on the availability of initial structural information; only the incorporation of a core constraint in Glide yields satisfactory predictions. To address this limitation, we developed a docking-free variant of MORLD that exploits receptor-derived shape similarity and pharmacophore alignment. Kernel-density estimation, convergence analysis, and SMARTS-based success-rate metrics confirmed that this Shape-Pharmacophore implementation autonomously generates chemically valid, SAR-consistent analogues of the reference compounds. Collectively, this work demonstrates a practical, structure-only driven paradigm for reinforcement-learning-based compound optimization, thereby extending the reach of AI-enabled drug design beyond traditional docking workflows.
Microbial Profiling of Buffalo Mozzarella Whey and Ricotta Exhausted Whey: Insights into Potential Probiotic Subdominant Strains Andrea Bonfanti, Romano Silvestri, Ettore Novellino, Gian Carlo Tenore, Elisabetta Schiano, Fortuna Iannuzzo, Massimo Reverberi, Luigi Faino, Marzia Beccaccioli, Francesca Sivori, Carlo Giuseppe Rizzello, Cristina Mazzoni Microorganisms, 2025 Buffalo mozzarella cheese whey (CW) and ricotta cheese exhausted whey (RCEW) are valuable by-products of the Mozzarella di Bufala Campana PDO production chain. This study characterized their microbial communities using an integrated culture-dependent and -independent approach. Metabarcoding analysis revealed that the dominance of lactic acid bacteria (LAB), including Streptococcus thermophilus, Lactobacillus delbrueckii, and Lactobacillus helveticus, alongside diverse heat-resistant yeasts such as Cyberlindnera jadinii. Culture-based isolation identified subdominant lactic acid bacteria strains, not detected by sequencing, belonging to Leuconostoc mesenteroides, Enterococcus faecalis, and Enterococcus durans. These strains were further assessed for their probiotic potential. E. faecalis CW1 and E. durans RCEW2 showed tolerance to acidic pH, bile salts, and lysozyme, as well as a strong biofilm-forming capacity and antimicrobial activity against Bacillus cereus and Staphylococcus aureus. Moreover, bile salt resistance suggests potential functionality in cholesterol metabolism. These findings support the potential use of CW and RCEW as reservoirs of novel, autochthonous probiotic strains and underscore the value of regional dairy by-products in food biotechnology and gut health applications.
Unveiling an unexpected redox regulation of the folding, function and inhibition in the phosphotyrosine binding domain of FRS2 Valeria Pennacchietti, Livia Pagano, Mariana Di Felice, Julian Toso, Marianna Bufano, Antonio Coluccia, Romano Silvestri, Riccardo Capelli, Carlo Camilloni, Francesca Malagrinò, Angelo Toto, Stefano Gianni International Journal of Biological Macromolecules, 2025 Protein-protein interaction domains are essential for cellular homeostasis and the regulation of various molecular pathways, mediating highly specific and reversible binding events. The PhosphoTyrosine-Binding domains (PTB) play a pivotal role in regulating several cellular events, by recognizing phosphorylated and, in some cases, non-phosphorylated ligands. In this study we investigated the folding and functional properties of the PTB domain of FRS2 (Fibroblast growth factor receptor substrate 2) under oxidative and reductive experimental conditions. Results demonstrate a surprising and previously undetected role of a disulfide bond between Cys61 and Cys80 residues in such events. Through an extensive site-directed mutagenesis we demonstrated that the presence/absence of such disulfide bridge, although not changing dramatically the overall structure of the domain, significantly influence its dynamic properties by rewiring a subtle energetic network stabilizing the domain. These effects result in remodulating its binding properties with phosphorylated and unphosphorylated peptides. Molecular dynamics simulations further elucidated how the oxidative/reductive conditions modulate the dynamics of the domain. Finally, we identified lead inhibitory compounds with different efficacy observed across the oxidized and reduced states of the PTB domain. Altogether, these findings provide novel insights for understanding the mechanism of regulation of the function of the PTB domain of FRS2.
Design and synthesis of novel thioether analogs as promising antiviral agents: In vitro activity against enteroviruses of interest Hugo Roux, Franck Touret, Antonio Coluccia, Pietro Scio, Hawa Sophia Bouzidi, Carole di Giorgio, Florence Gattacceca, Omar Khoumeri, Romano Silvestri, Patrice Vanelle, Manon Roche European Journal of Medicinal Chemistry, 2025 The Enterovirus genus contains two major subgroups: rhinovirus (RV) species A-C and enterovirus (EV) ones A-D. While RV only infects the respiratory system, the EV can cause a wide variety of diseases, ranging from non-specific febrile illness to severe neurologic complications. To date, no curative treatments are commercially available. Our research team had recently developed EV-A71 inhibitors. To improve their activity and broaden their spectrum, we performed optimization of the structure following an iterative cycle of chemical modulations. As a result, we obtained two broad-spectrum inhibitors with micromolar activity against these 3 types of viruses ( OM1260 : EC 50 (MRC-5, EV-A71) = 1.15 μM; EC 50 (RD, EV-A71) = 4.38 μM; EC 50 (MRC-5, E30) = 0.41 μM; EC 50 (MRC-5, CVA24) = 1.15 μM; HR-568 : EC 50 (MRC-5, EV-A71) = 3.25 μM; EC 50 (RD, EV-A71) = 1.53 μM; EC 50 (MRC-5, E30) = 0.40 μM; EC 50 (MRC-5, CVA24) = 1.22 μM). Docking studies shed light on structure-activity relationships, while time-of-drug addition assays confirmed their intervention during the early step of viral replication. Eventually, some pharmacokinetic modelling has been carried out to evaluate their druggability. All these results showed that OM1260 and HR-568 are promising candidates for further development. • High-yielding reaction thanks to 2 optimized synthesis strategies. • Fused bicycles in toe-end side to broaden the hydrophobic interactions with the target. • Description of new derivatives with micromolar/sub micromolar activity. • Innovative and rigorous methods to evaluate activity against EV-A71, E30, and CVA24 in 2 cell lines. • Modelling of physicochemical and pharmacokinetic parameters of the most promised compounds.
New potent EV-A71 antivirals targeting capsid Hugo Roux, Franck Touret, Antonio Coluccia, Omar Khoumeri, Carole Di Giorgio, Chaimae Majdi, Pietro Sciò, Romano Silvestri, Patrice Vanelle, Manon Roche European Journal of Medicinal Chemistry, 2024
4-(3-Phenylsulfonylindol-2-yl)-1-(pyridin-2-yl)piperazinyl-methanones as Potent Inhibitors of both SARS-CoV-2 and HCoV-OC43 Viruses Michela Puxeddu, Manuela Donalisio, Joachim Jakob Bugert, Angela Corona, Paolo Cocomazzi, Mario Milani, Friederike Hucke, Irene Arduino, Francesca Esposito, Paolo Moretti, Maria Grazia Ortore, Marianna Nalli, Simone Manetto, Giulia Mazzoccanti, Chiara Bigogno, Giulio Dondio, Pietro Sciò, Antonio Coluccia, Matteo Fracella, Guido Antonelli, David Lembo, Enzo Tramontano, Romano Silvestri, Eloise Mastrangelo, Giuseppe La Regina ACS Infectious Diseases, 2024
Quinoline-based thiazolyl-hydrazones target cancer cells through autophagy inhibition Vladimir Ćurčić, Mateusz Olszewski, Natalia Maciejewska, Aleksandar Višnjevac, Tatjana Srdić‐Rajić, Vladimir Dobričić, Alfonso T. García‐Sosa, Sanja B. Kokanov, Jovana B. Araškov, Romano Silvestri, Roland Schüle, Manfred Jung, Milan Nikolić, Nenad R. Filipović Archiv Der Pharmazie, 2024
Novel N-(Heterocyclylphenyl)benzensulfonamide Sharing an Unreported Binding Site with T-Cell Factor 4 at the β-Catenin Armadillo Repeats Domain as an Anticancer Agent Marianna Nalli, Laura Di Magno, Yichao Wen, Xin Liu, Michele D’Ambrosio, Michela Puxeddu, Anastasia Parisi, Jessica Sebastiani, Andrea Sorato, Antonio Coluccia, Silvia Ripa, Fiorella Di Pastena, Davide Capelli, Roberta Montanari, Domiziana Masci, Andrea Urbani, Chiara Naro, Claudio Sette, Viviana Orlando, Sara D’Angelo, Stefano Biagioni, Chiara Bigogno, Giulio Dondio, Arianna Pastore, Mariano Stornaiuolo, Gianluca Canettieri, Te Liu, Romano Silvestri, Giuseppe La Regina ACS Pharmacology and Translational Science, 2023
Structural Investigations on Novel Non-Nucleoside Inhibitors of Human Norovirus Polymerase Gilda Giancotti, Giulio Nannetti, Gilda Padalino, Martina Landini, Nanci Santos-Ferreira, Jana Van Dycke, Valentina Naccarato, Usheer Patel, Romano Silvestri, Johan Neyts, Roberto Gozalbo-Rovira, Jésus Rodríguez-Díaz, Joana Rocha-Pereira, Andrea Brancale, Salvatore Ferla, Marcella Bassetto Viruses, 2023
Induction of Ferroptosis in Glioblastoma and Ovarian Cancers by a New Pyrrole Tubulin Assembly Inhibitor Michela Puxeddu, Jianchao Wu, Ruoli Bai, Michele D’Ambrosio, Marianna Nalli, Antonio Coluccia, Simone Manetto, Alessia Ciogli, Domiziana Masci, Andrea Urbani, Cinzia Fionda, Sonia Coni, Rosa Bordone, Gianluca Canettieri, Chiara Bigogno, Giulio Dondio, Ernest Hamel, Te Liu, Romano Silvestri, Giuseppe La Regina Journal of Medicinal Chemistry, 2022
Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia Michela Puxeddu, Hongliang Shen, Ruoli Bai, Antonio Coluccia, Marianna Bufano, Marianna Nalli, Jessica Sebastiani, Diego Brancaccio, Eleonora Da Pozzo, Chiara Tremolanti, Claudia Martini, Viviana Orlando, Stefano Biagioni, Maria Stefania Sinicropi, Jessica Ceramella, Domenico Iacopetta, Addolorata Maria Luce Coluccia, Ernest Hamel, Te Liu, Romano Silvestri, Giuseppe La Regina European Journal of Medicinal Chemistry, 2021
CXCR4 antagonism sensitizes cancer cells to novel indole-based MDM2/4 inhibitors in glioblastoma multiforme Simona Daniele, Valeria La Pietra, Rebecca Piccarducci, Deborah Pietrobono, Chiara Cavallini, Vincenzo Maria D'Amore, Linda Cerofolini, Stefano Giuntini, Pasquale Russomanno, Michela Puxeddu, Marianna Nalli, Martina Pedrini, Marco Fragai, Claudio Luchinat, Ettore Novellino, Sabrina Taliani, Giuseppe La Regina, Romano Silvestri, Claudia Martini, Luciana Marinelli European Journal of Pharmacology, 2021
Targeting the interaction between the SH3 domain of Grb2 and Gab2 Francesca Malagrinò, Antonio Coluccia, Marianna Bufano, Giuseppe La Regina, Michela Puxeddu, Angelo Toto, Lorenzo Visconti, Alessio Paone, Maria Chiara Magnifico, Francesca Troilo, Francesca Cutruzzolà, Romano Silvestri, Stefano Gianni Cells, 2020
Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents Antonio Coluccia, Giuseppe La Regina, Valentina Naccarato, Marianna Nalli, Viviana Orlando, Stefano Biagioni, Maria Laura De Angelis, Marta Baiocchi, Candice Gautier, Stefano Gianni, Fiorella Di Pastena, Laura Di Magno, Gianluca Canettieri, Addolorata Maria Luce Coluccia, Romano Silvestri ACS Medicinal Chemistry Letters, 2019
New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors Giuseppe La Regina, Ruoli Bai, Antonio Coluccia, Valentina Naccarato, Valeria Famiglini, Marianna Nalli, Domiziana Masci, Annalisa Verrico, Paola Rovella, Carmela Mazzoccoli, Eleonora Da Pozzo, Chiara Cavallini, Claudia Martini, Stefania Vultaggio, Giulio Dondio, Mario Varasi, Ciro Mercurio, Ernest Hamel, Patrizia Lavia, Romano Silvestri European Journal of Medicinal Chemistry, 2018
Bax Activation Blocks Self-Renewal and Induces Apoptosis of Human Glioblastoma Stem Cells Simona Daniele, Deborah Pietrobono, Barbara Costa, Mariateresa Giustiniano, Valeria La Pietra, Chiara Giacomelli, Giuseppe La Regina, Romano Silvestri, Sabrina Taliani, Maria Letizia Trincavelli, Federico Da Settimo, Ettore Novellino, Claudia Martini, Luciana Marinelli ACS Chemical Neuroscience, 2018
Arginine- and lysine-rich peptides: Synthesis, characterization and antimicrobial activity Adriano Mollica, Giorgia Macedonio, Azzurra Stefanucci, Roberto Costante, Simone Carradori, Valentina Cataldi, Mara Di Giulio, Luigina Cellini, Romano Silvestri, Cesare Giordano, Anita Scipioni, Stefano Morosetti, Pasqualina Punzi, Sako Mirzaie Letters in Drug Design and Discovery, 2018
A high-throughput screening of a chemical compound library in ovarian cancer stem cells F. Ricci, L. Carrassa, M. S. Christodoulou, D. Passarella, B. Michel, R. Benhida, N. Martinet, A. Hunyadi, E. Ioannou, V. Roussis, L. Musso, S. Dallavalle, R. Silvestri, N. Westwood, M. Mori, C. Ingallina, B. Botta, E. Kavetsou, A. Detsi, Z. Majer, F. Hudecz, S. Bosze, B. Kaminska, T.V. Hansen, P. Bertrand, C. M. Athanassopoulos, G. Damia Combinatorial Chemistry and High Throughput Screening, 2018
3-Aroyl-1,4-diarylpyrroles Inhibit Chronic Myeloid Leukemia Cell Growth through an Interaction with Tubulin Giuseppe La Regina, Ruoli Bai, Antonio Coluccia, Valeria Famiglini, Sara Passacantilli, Valentina Naccarato, Giorgio Ortar, Carmela Mazzoccoli, Vitalba Ruggieri, Francesca Agriesti, Claudia Piccoli, Tiziana Tataranni, Marianna Nalli, Andrea Brancale, Stefania Vultaggio, Ciro Mercurio, Mario Varasi, Concetta Saponaro, Sara Sergio, Michele Maffia, Addolorata Maria Luce Coluccia, Ernest Hamel, Romano Silvestri ACS Medicinal Chemistry Letters, 2017
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer Giuseppe La Regina, Ruoli Bai, Antonio Coluccia, Valeria Famiglini, Sveva Pelliccia, Sara Passacantilli, Carmela Mazzoccoli, Vitalba Ruggieri, Annalisa Verrico, Andrea Miele, Ludovica Monti, Marianna Nalli, Romina Alfonsi, Lucia Di Marcotullio, Alberto Gulino, Biancamaria Ricci, Alessandra Soriani, Angela Santoni, Michele Caraglia, Stefania Porto, Eleonora Da Pozzo, Claudia Martini, Andrea Brancale, Luciana Marinelli, Ettore Novellino, Stefania Vultaggio, Mario Varasi, Ciro Mercurio, Chiara Bigogno, Giulio Dondio, Ernest Hamel, Patrizia Lavia, Romano Silvestri Journal of Medicinal Chemistry, 2015
Pharmacological folding chaperones act as allosteric ligands of Frizzled4 Serena F Generoso, Mariateresa Giustiniano, Giuseppe La Regina, Sara Bottone, Sara Passacantilli, Salvatore Di Maro, Hilde Cassese, Agostino Bruno, Massimo Mallardo, Monica Dentice, Romano Silvestri, Luciana Marinelli, Daniela Sarnataro, Stefano Bonatti, Ettore Novellino, Mariano Stornaiuolo Nature Chemical Biology, 2015
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer Giuseppe La Regina, Ruoli Bai, Antonio Coluccia, Valeria Famiglini, Sveva Pelliccia, Sara Passacantilli, Carmela Mazzoccoli, Vitalba Ruggieri, Lorenza Sisinni, Alessio Bolognesi, Whilelmina Maria Rensen, Andrea Miele, Marianna Nalli, Romina Alfonsi, Lucia Di Marcotullio, Alberto Gulino, Andrea Brancale, Ettore Novellino, Giulio Dondio, Stefania Vultaggio, Mario Varasi, Ciro Mercurio, Ernest Hamel, Patrizia Lavia, Romano Silvestri Journal of Medicinal Chemistry, 2014
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors Giuseppe La Regina, Ruoli Bai, Whilelmina Maria Rensen, Erica Di Cesare, Antonio Coluccia, Francesco Piscitelli, Valeria Famiglini, Alessia Reggio, Marianna Nalli, Sveva Pelliccia, Eleonora Da Pozzo, Barbara Costa, Ilaria Granata, Amalia Porta, Bruno Maresca, Alessandra Soriani, Maria Luisa Iannitto, Angela Santoni, Junjie Li, Marlein Miranda Cona, Feng Chen, Yicheng Ni, Andrea Brancale, Giulio Dondio, Stefania Vultaggio, Mario Varasi, Ciro Mercurio, Claudia Martini, Ernest Hamel, Patrizia Lavia, Ettore Novellino, Romano Silvestri Journal of Medicinal Chemistry, 2013
Apple can act as anti-aging on yeast cells Vanessa Palermo, Fulvio Mattivi, Romano Silvestri, Giuseppe La Regina, Claudio Falcone, Cristina Mazzoni Oxidative Medicine and Cellular Longevity, 2012
PYRROLO[1,2-b][1,2,5]BENZOTHIADIAZEPINES (PBTDs) induce apoptosis in K562 cells Gabriella Marfe, Carla Di Stefano, Romano Silvestri, Elisabetta Abruzzese, Gianfranco Catalano, Livia Di Renzo, Giuseppe Filomeni, Ezio Giorda, Giuseppe La Regina, Emanuela Morgante, Maria Rosa Ciriolo, Matteo Antonio Russo, Sergio Amadori, Paola Sinibaldi-Salimei BMC Cancer, 2007
Arylthioindoles, potent inhibitors of tubulin polymerization Gabriella De Martino, Giuseppe La Regina, Antonio Coluccia, Michael C. Edler, Maria Chiara Barbera, Andrea Brancale, Elizabeth Wilcox, Ernest Hamel, Marino Artico, Romano Silvestri Journal of Medicinal Chemistry, 2004
A simplified synthesis of ethyl 5-chloro-4-fluoro-1H-indole-2-carboxylate and ethyl 5-chloro-6-fluoro-1H-indole-2-carboxylate Organic Preparations and Procedures International, 2002
Anti-HIV-1 NNRT agents: Acylamino Pyrryl Aryl Sulfones (APASs) as truncated analogues of tricyclic PBTDs Medicinal Chemistry Research, 2002
Sulfone derivatives with anti-HIV activity Farmaco, 1997
Synthesis and anti-HIV activity of 10,11-dihydropyrrolo [1,2- b][1,2,5]benzothiadiazepine-11-acetic acid 5,5-dioxide derivatives and related compounds Farmaco, 1996
Heterocycles with a benzothiadiazepine moiety. 2. Synthesis of 2-methyl-1,3,4,14b-tetrahydro-2H-pyrazino[2,1-d]pyrrolo-[1,2-b][1,2,5] benzothiadiazepine 10,10-dioxide (tiaaptazepine) Journal of Heterocyclic Chemistry, 1994
Sperner's lemma and robust machines Proceedings of the Eighth Annual Structure in Complexity Theory Conference, 1993
Antifungal agents. VI. In vitro antifungal activities of halobenzoyl esters of cis- and trans-[2-(1,1'-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan- 4-yl]carbinols Farmaco, 1993
Researches on psychotropic agents. IV. Synthesis and neuropsychopharmacological effects of 1,3,4,14 b-tetrahydro-10-methyl-2H,10H-pyrazino[2,1-d]pyrrolo[1,2-b][1,2,5]benz otriazepine and its derivatives Farmaco, 1992
Research on psychotropic agents. III. Antidepressant activity and neuropsychobehavioural effects of new 5H-pyrrolo[1,2-b][1,2,5] benzotriazepine derivatives Farmaco, 1990
Non-steroidal antiinflammatory agents. VIII. Synthesis and antiinflammatory activity of 5-methyl-10,11-dihydro-5H-pyrrolo [1,2-b][1,2,5]benzotriazepine-11-acetic acid and its 10-aroyl derivatives Farmaco, 1990
5-Aroyl-5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepin-4-carboxilic acids: Synthesis and analgesic and neurobehavioural activity Farmaco, 1989
Synthesis, neuropsychopharmacological effects and analgesic-antiinflammatory activities of pyrrole analogues of lefetamine Farmaco, 1989
Researches on antibacterial and antifungal agents. IX - Pyrrole analogues of bifonazole with potent antifungal activities Farmaco Edizione Scientifica, 1988
Non-steroidal antiinflammatory agents. V. Synthesis of 1-aryl-5-(l-pyrryl)-pyrazolyl-4-acetic acids with potential antiinflammatory activity Farmaco Edizione Scientifica, 1988
Potential antitumor agents. 1. Synthesis of pyrroloindazole derivatives related to the pyrroloindole moieties of the antitumor antibiotic CC-1065 Farmaco Edizione Scientifica, 1987
Research on antibacterial and antifungal agents: VII. Synthesis of (1-pyrryl)methylquinolones Farmaco Edizione Scientifica, 1987
Potential antitumor agents. II. Lappin intramolecular cyclization of diethyl 3-carbazolylaminomethylenemalonate: A structure assignment Farmaco Edizione Scientifica, 1987
Research on new psychotropic agents. I. Synthesis and pharmacological activity of derivatives of 5H-imidazo[2,1-c] [1,4]benzodiazepine Farmaco Edizione Scientifica, 1985
