Publications
“From green innovations in oligopeptides to oligonucleotides sustainable synthesis: differences and synergies in TIDES chemistry.” Ferrazzano,L.; Corbisiero,D.; Tolomelli,A.; Cabri,W. Green Chemistry 2023,25, 1217.
“Speeding up sustainable solution-phase peptide synthesis using T3P® as a green coupling reagent: methods and challenges.” Mattellone,A.; Corbisiero, D.; Ferrazzano,L.; Cantelmi,P.; Martelli,G.; Palladino,C.; Tolomelli,A.; Cabri,W. Green Chemistry 2023, 25, 2563.
“New Mechanistic Insights into the Copper-free Heck–Cassar–Sonogashira cross-coupling reaction.” Palladino,C.; Fantoni, T.; Ferrazzano, L.; Muzzi,B.; Ricci,A.; Tolomelli,A.; Cabri,W. ACS Catalysis 2023,13, 12048−12061.
“Copper-Free Heck−Cassar−Sonogashira and Suzuki−Miyaura Reactions of Aryl Chlorides: A Sustainable Approach” Palladino, C.; Fantoni,T.; Ferrazzano,L-; Tolomelli,A.; Cabri,W. ACS SustainableChem.Eng. 2023,11, 15994−16004.
“Fast Solution-Phase and Liquid-Phase Peptide Syntheses (SolPSS and LPPS) Mediated by Biomimetic Cyclic Propylphosphonic Anhydride (T3P®) Mattellone,A.; Corbisiero,D.; Cantelmi,P.; Martelli,G.; Palladino,C.; Tolomelli, A.; Cabri,W. ; Ferrazzano,L. Molecules 2023, 28, 7183.
“Dimethyl carbonate as a green alternative to acetonitrile in reversed-phase liquid chromatography. Part I: Separation of small molecules.” Felletti,S.; Spedicato,M.; Bozza,d.; De Luca,C.; Presini,F:; Giovannini,P.; Carraro,M.; Macis,M.; Cavazzini,A:; Catani,M.; Ricci,A.; Cabri,W. J. of Chromatography A 2023, 1712, 464477.
“Dimethyl carbonate as a green alternative to acetonitrile in reversed-phase liquid chromatography. Part II: purification of a therapeutic peptide.” Bozza.D.; De Luca, C.; Felletti.ì, S.; Spedicato, M.; Presini F.; Giovannini, P.P.; Carraro, M.; Macis, M.; Cavazzini, A.; Catani, M.; Ricci, A.; Cabri, W. J. of Chromatography A 2023, 1713, 464530.
“Application of Af4-Multidetection to Liraglutide in Its Formulation: Preserving and Representing Native Aggregation” Marassi,V.; Macis,M.; Giordani,S.; Ferrazzano,L.; Tolomelli,A.; Roda,B.; Zattoni,A.; Ricci,A.; Reschiglian,P.; Cabri,W. Molecules 2022,27,5485
“Carbodiimide-Mediated Beckmann Rearrangement of Oxyma-B as a Side Reaction in Peptide Synthesis.” Orlandin,A.; Guryanov,I.; Ferrazzano,L.; Biondi,B.; Biscaglia,F:; Storti,C.; Rancan,M.; Formaggio,F.; Ricci,A.; Cabri,W. Molecules 2022, 27, 4235
“Peptides Drug Discovery and Process Development Perspective.” Fantoni,T.; Tolomelli,A.; Cabri,W. Chemistry Today 2022, 40, 40-45.
Benefits of a Mixed-Mode Stationary Phase to Address the Challenging Purification of an Industrially Relevant Peptide: A Proof-of-Concept Study” Lievore,G.; Bozza,D,; Catani,M.; Cavazzini,A.; Chenet,T.; Pasti,L.; Ferrazzano,L.; Cabri,W.; Macis,M.; Ricci,A.; De Luca,C.; Felletti,S. Separations 2022, 9,125.
“A New Approach to Supramolecular Structure Determination in Pharmaceutical Preparation of Self-Assembling Peptides: A Case Study of Lanreotide Autogel”. Grimaldi, M.; Santoro,A.; Buonocore,M.; Crivaro,C.; Funicello,N.; Sublimi Saponetti,M.; Ripoli,C.; Rodriquez,M., De Pasquale,S.; Bobba,F.; Ferrazzano,L.; Cabri,W., Maria D’Ursi,A.; Ricci,A. Pharmaceutics 2022,14,681
“A translation of the twelve principles of green chemistry to guide the development of cross-coupling reactions” Fantoni,T.; Tolomelli,A.; Cabri,W. Catalysis Today 2022, 397-399,265-271
"Sustainability in peptide chemistry: current synthesis and purification technologies and future challenges" Ferrazzano,L.; Catani,M.; Cavazzini,A.; Martelli,G.; Corbisiero,D.; Cantelmi,P.; Fantoni,T.; Mattellone,A.; De Luca,C.; Felletti,S.; Cabri,W:; Tolomelli,A. Green Chemistry 2022, 24,975
“Copper(II) Lysinate and Pseudoproline Assistance in the Convergent Synthesis of the GLP-1 Receptor Agonists Liraglutide and Semaglutide” Guryanov,I.; Orlandin,A., De Paola,I.; Viola,A.; Biondi,B.; Badocco,D.; Formaggio,F.; Ricci,A.; Cabri,W. Org. Process Res. Dev. 2021, 25, 7, 1598–1611
“Replacing piperidine in Solid Phase Peptide Synthesis: effective Fmoc removal by alternative bases.” Martelli,G.; Cantelmi,P.; Palladino,C.; Mattellone,A.; Corbisiero,D.; Fantoni,T.; Tolomelli,A.; Cabri,W.; Ferrazzano,L. Green Chemistry 2021, 23, 8096
“Downstream Processing of Therapeutic Peptides by Means of Preparative Liquid Chromatography” De Luca,C.; Lievore,G.; Bozza,D.; Buratti,A.; Cavazzini,A.; Ricci,A.; Macis,M.; Cabri,W.; Felletti,S.; Catani,M. Molecules, 2021, 26,4688.
“The Role of Adsorption and pH of the Mobile Phase on the Chromatographic Behavior of a Therapeutic Peptide.” Felletti,S.; De Luca,C.; Lievore,G., Buratti,A.; Bozza,D.; Macis,M.; Ricci,A.; Cabri,W.; Cavazzini,A.; Catani,M. LCGC NA 2021, 39, 14-20.
“Expanding the Use of Dynamic Electrostatic Repulsion Reversed-Phase Chromatography: An Effective Elution Mode for Peptides Control and Analysis.” Mazzoccanti,G.; Manetto,S.; Bassan,M.; Macis,M.; Iazzetti,A.; Cabri,W.; Ricci,A.; Gasparrini,F. Molecules 2021, 26, 4348.
“Therapeutic Peptides Targeting PPI in Clinical Development: Overview, Mechanism of Action and Perspectives.” W.Cabri,P. Cantelmi, D. Corbisiero, T. Fantoni, L. Ferrazzano, G. Martelli, A. Mattellone, A.Tolomelli Frontiers in Mol Bios. 2021, 8, art.6975586
“Steps towards sustainable Solid Phase Peptide Synthesis: use and recovery of N-octyl pyrrolidone.” Green Chemistry 2021, 23, 4095–4106
“Palladium catalyst recycling for Heck‐Cassar‐Sonogashira cross coupling reactions in the green N‐hydrohyethyl pyrrolidone/water/N,N,N’,N’‐tetramethyl guanidine blend.” ChemSusChem 2021, 14, 2591–2600.
“Process Intensification for the Purification of Peptidomimetics: The Case of Icatibant through Multicolumn Countercurrent Solvent Gradient Purification (MCSGP).” De Luca,C.; Felletti,S.; Bozza,D.; Lievore,G.; Morbidelli,M.; Sponchioni,M.; Cavazzini,A.; Catani,M.; Cabri,W.; Macis,M.; Ricci,A. Ind. Eng. Chem. Res. 2021, 60, 6826−6834.
“Fast Heck−Cassar−Sonogashira (HCS) Reactions in Green Solvents” Ferrazzano L; Marteli G; Fantoni T; Daka A; Corbisiero D; Viola A; Ricci A; Cabri W; Tolomelli A Organic Letters 2020,22,3969-3973
"High-throughput enantioseparation of Nα-fluorenylmethoxycarbonyl proteinogenic amino acids through fast chiral chromatography on zwitterionic-teicoplanin stationary phases" Mazzoccanti G; Manetto S; Ricci A; Cabri W; Orlandin A; Catani M; Felletti S; Cavazzini A.; Ye M; Ritchie H; Villani C; Gasparrini F. Journal of Chromatography A 2020,1624,461235
"From batch to continuous chromatographic purification of a therapeutic peptide through Multicolumn Countercurrent Solvent Gradient Purification (MCSGP)" De Luca, C; Felletti S ; Lievore G; Buratti A; Vogg S; Morbidelli M; Cavazzini A; Catani M; Macis M; Ricci A; Cabri , W. Journal of Chromatography A 2020,1625,461304
"Ganoderma Lucidum Ethanol Extract Enhance Re-epithelialization and prevent Keratinocytes from Free Radical Injury" Abate,M.; Pepe,G.; Randino,R.; Pisanti,S.; Basilicata,M.G.; Covelli,V.; Bifulco,M.; Cabri,W.; D'Ursi,A.; Campiglia,A.; Rodriquez,M. Pharmaceuticals 2020,13,224-239
"Integrin-mediated adhesive properties of neutrophils are reduced by hyperbaric oxygen therapy in patients with chronic non-healing wound." M.Baiula, R.Greco, L.Ferrazzano, A.Caligiana, K.Hoxha, D.Bandini, P.Longobardi, S.Spampinato, A. Tolomelli* PlosOne 2020,15,e0237746
"Ampicillin sodium: isolation, identification and synthesis of the last unknown impurity after 60 years of clinical use." A.Tolomelli1 A.Ricci, A. Viola, M.Bassan, L.Ferrari, L. Ferrazzano. G.Martelli, A. Mattellone, W. Cabri * Journal of Pharmaceutical and Biomedical Analysis, 2020,123,1-6
“Side chain effect in the modulation of αvβ3/α5β1 integrin activity via clickable isoxazoline-RGD-mimetics: development of molecular delivery systems.” L.Ferrazzano, D.Corbisiero, E.Potenza, M.Baiula, S.D.Dattoli, S.Spampinato, L.Belvisi, M.Civera and A.Tolomelli Scientific Report 2020,10.7410.
"Pharmaceutical Green Chemistry in Peptide Synthesis – A Snapshot on the Role of Solvents in SPPS" G. Martelli, L. Ferrazzano*, A. Tolomelli, A. Ricci, W. Cabri* Chemistry Today, 2020, 38, 14-17.
"Overcoming Chemical Challenges in the Solid-Phase Synthesis of High-Purity GnRH Antagonist Degarelix. Part 2", I. Guryanov, A. Orlandin, A. Viola, B. Biondi, F. Formaggio, A. Ricci, W.Cabri, OPRD, .2020, 24, 274-278.
Boosting basic-peptide separation through dynamic electrostatic-repulsion reversed-phase (d-ERRP) liquid chromatography, G. Mazzoccanti, S. Manetto, M. Bassan, A. Foschini, A. Orlandin, A. Ricci, W. Cabri,O. H. Ismail, M.Catani, A. Cavazzini, F. Gasparrini RSC Adv., 2020, 10, 12604-12610.
"Modeling the nonlinear behavior of a bioactive peptide in reversed-phase gradient elution chromatography", C. De Luca, S. Felletti, M. Macis, W. Cabri, G. Lievore, T. Chenet, L. Pasti, M.Morbidelli, A. Cavazzini, M.Catani, A. Ricci, Journal of Chromatography A , 2020, 460789.
"Fluorene benzothiazole co-oligomer based acqueus self-assembled nanoparticles" J. Schill, L. Ferrazzano, A. Tolomelli, APHJ. Schenning, L. Brunsweld RCS Advance 2020,10,444 DOI: 10.1039/c9ra09015k
"Two Dimensional UV Spectroscopy: a new insight into the structure and dynamics of biomolecules" R. Borrego-Varillas, A. Nenov, L. Ganzer, A. Oriana, C. Manzoni, A. Tolomelli, I. Rivalta, s. Mukamel, M. Garavelli, G. Cerullo Chemical Science, 2019, 10,9907 DOI: 10/1039/c9sc03871j
"Overcoming chemical challenges in the solid-phase synthesis of high-purity GnRH antagonist Degarelix" I. Guryanov, A. Orlandin, A: Viola, B.Biondi, D:Badocco, F: Formaggio, A.Ricci, W. Cabri. OPRD 2019,23, 2746.
“Natural Occurring and Engineered Enzymes for Peptide Ligation and Cyclization” N. Timo, A, Toplak, M. Schmidt, A. Ricci, W. Cabri Frontiers in Chemistry 2019,7,829.
"Synthesis of alpha/beta dipeptides containing linear or cyclic alpha-dehydro-beta amino acids as scaffolds as bioactive compounds" L. Ferrazzano, D. Corbisiero, R. Greco, E. Potenza, G. De Serlis, A. Garelli, A. Tolomelli Amino Acids 2019,51,1475 DOI: 10.1007/s00726-019-02782-7
"Green Solvent Mixtures for Solid-Phase Peptide Synthesis: A Dimethylformamide-Free Highly Efficient Synthesis of Pharmaceutical-Grade Peptides", L. Ferrazzano, D. Corbisiero, G. Martelli, A. Tolomelli, A. Viola, A. Ricci, W. Cabri, ACS Sustainable Chem. Eng. 2019, ASAP, https://doi.org/10.1021/acssuschemeng.9b01766
"Novel insights into the chemistry of an old medicine: A general degradative pathway for penicillins from a piperacillin/tazobactam stability study", A. Viola, L. Ferrazzano, G. Martelli, L. Cerisoli, A. Ricci, A.Tolomelli, W.Cabri, Eur. J. Pharm. Sci. 2019, 136, 104957 https://doi.org/10.1016/j.ejps.2019.104957.
"Novel Ligands Targeting alpha(4)beta(1) Integrin: Therapeutic Applications and Perspectives", M. Baiula, S. Spampinato, L. Gentilucci, A.Tolomelli Frontiers in Chemistry, 2019, 7, 489, DOI: 10.3389/fchem.2019.00489.
“Stable and Biocompatible Monodispersion of C-60 in Water by Peptides” M. Di Giosia, F. Nicolini, L. Ferrazzano, A. Solda, F. Valle, A. Cantelli, T.D.Marforio, A. Bottoni, F. Zerbetto, M. Montalti, S. Rapino, A. Tolomelli*, M. Calvaresi* Bioconj. Chem. 2019, 30,808-814, DOI: 10.1021/acs.bioconjchem.8b00916
“Synthesis of Enantiopure Isosteres of Amino Acids Containing a Quaternary Stereocenter: Experimental and Computational Evaluation of a Novel Class of Atropisomers” P. Amabili, A. Amici, G. Campisi, G. Guerra, M. Monari, M. Orena, F. Piccinelli, S. Rinaldi, A. Tolomelli, Eur. J. Org. Chem.,2018, 46, 6524-6536. DOI: 10.1002/ejoc.201801213.
“Novel Antagonist Targeting Ephb1 Receptor”, G. Vaca, A. Bedini, A.Tolomelli, S. Spampinato, BASIC & CLIN.PHARM. TOXIC. 2018, 123 SI Pages: 86-86.
“Novel Rgd-Ligands Differently Modulate Alpha 5 Beta 1 Integrin-Mediated Adhesion, Signaling And Trafficking” M .Baiula, A. Tolomelli, L. Ferrazzano, G. Giacomini, P. Galletti, S. Spampinato BASIC & CLIN.PHARM. TOXIC. 2018, 123 SI Pages:: 72-72
"4-Substituted prolines, useful reagents in enantioselective synthesis and conformational restraints in bioactive peptidomimetics design", A. Tolomelli, A., L. Ferrazzano, R. Amoroso, Aldrichimica Acta 2017, 50(1), 3-15.
“Can Integrin Agonists Have Cards to Play against Cancer? A Literature Survey of Small Molecules Integrin Activators” A . Tolomelli, P. Galletti, M. Baiula, D. Giacomini, CANCERS, 2017, 9, 78, DOI: 10.3390/cancers9070078.
“New isoxazolidinone and 3,4-dehydro-β-proline derivatives as antibacterial agents and MAO-inhibitors: A complex balance between two activities” L. Ferrazzano, A.Viola, E. Lonati, A. Bulbarelli, R. Musumeci, C. Cocuzza, M. Lombardo, A. Tolomelli, Eur. J. Med. Chem. 2016, 124, 906-919, ISSN: 0223-5234, doi:10.1016/j.ejmech.2016.09.007.
“One-Pot Two-Step Microwave-Assisted Synthesis of Alkylidene Acetoacetamido Esters, Useful Intermediates for β-Dehydropeptides” A. Viola, L.Ferrazzano, R. Greco, L. Cerisoli, J. Caldi and A. Tolomelli, Eur. J. Org. Chem., 2016, 19, 3217–3222. DOI: 10.1002/ejoc.201600376.
“Spectroscopic fingerprints of DNA/RNA pyrimidine nucleobases in third-order nonlinear electronic spectra”, A. Giussani, J.Segarra-Mart, A. Nenov, I. Rivalta, A. Tolomelli, S. Mukamel, M.Garavelli, Theoretical Chemistry Accounts, 2016, 135(5), 1-18.
“Highly stable atropisomers by electrophilic amination of a chiral γ‑lactam within the synthesis of an elusive conformationally restricted analogue of α‑methylhomoserine”, P.Amabili, A. Amici, A. Civitavecchia, B. Maggiore, M. Orena, S. Rinaldi, A. Tolomelli, Amino Acids, 2016, 48, 461-478. DOI 10.1007/s00726-015-2100-4.
“Integrin Ligands with a/b-Hybrid Peptide Structure: Design, Bioactivity, Stability, and Conformational Aspects”, R. De Marco, A. Tolomelli, E. Juaristi, L. Gentilucci, Med. Res. Rev., 2016, 36(3), 389-424.
“A review of strategies for the development of Pro-Leu, Pro-Ile, and Pro-Val chimeras and other alkyl prolines for drug discovery”, A.Tolomelli, A. Ammazzalorso, I. Bruno, R. Amoroso, Current bioactive compounds, 2016, 12, 146-160, DOI: 10.2174/1573407212666160511155230.
“Dehydro-b-proline containing peptidomimetics as selective a4b1 integrin antagonists: a stereochemical recognition in ligand-receptor interaction”, A. Tolomelli, M. Baiula, A. Viola, L. Ferrazzano, L.Gentilucci, S. D. Dattoli,] S. Spampinato, E. Juaristi, M. Escudero, ACS Med, Chem. Lett. , 2015, 6, 701-706.
“Design and Synthesis of avb3 and a5b1 integrin ligands as delivery systems for fluorescent molecules”, ”, A. Tolomelli, L.Gentilucci, , A. Viola, S. D. Dattoli, M. Baiula, S. Spampinato, K. Petkau-Milroy, L. Brunsveld, La Chimica e l’Industria, 2014, 96 (5/6), 56-58.
“An improved microwave assisted protocol for Yonemitsu-type trimolecular condensation”, A. Viola, L. Ferrazzano, G. Martelli, S. Ancona, L.Gentilucci, A. Tolomelli, Tetrahedron 2014, 70, 6781–6788, doi: 10.1016/j.tet.2014.07.062
“Synthesis and assay of retro-alpha 4 beta 1 integrin-targeting motifs” S.D. Dattoli, R. De Marco, M. Baiula, S. Spampinato, A. Greco, A. Tolomelli, L. Gentilucci Eur. J. Org. Chem. 2014, 225-232 .
“Convenient Synthesis of the Antibiotic Linezolid via an Oxazolidine-2,4-dione Intermediate Derived from the Chiral Building Block Isoserine”, A.Greco; R. De Marco; S. Tani; D. Giacomini; P. Galletti; A. Tolomelli; E. Juaristi; L. Gentilucci; Eur. J. Org.Chem., 2014, 7614-7620.
“Targeting integrins avb3 and a5b1 with new b-lactam derivatives” P. Galletti, R. Soldati, M.Pori, M. Durso, A. Tolomelli, L. Gentilucci, S. D. Dattoli, M.Baiula, Santi Spampinato, Daria Giacomini Eur. J. Med. Chem. 2014, 83, 284–293.
“Controlled Solid Phase Peptide Bond Formation Using N-Carboxyanhydrides and PEG Resins in Water”, R. De Marco, A. Tolomelli, A. Greco, L. Gentilucci ACS Sus. Chem. Eng. 2013, 1, 566-569.
“Modulation of avb3- and a5b1-integrin-mediated adhesion by dehydro-beta-amino acids containing peptidomimetics.” A. Tolomelli, M. Baiula, L. Belvisi, A. Viola, L. Gentilucci, S. Troisi, S. D. Dattoli, Samantha S. Spampinato, M. Civera, E. Juaristi, M. Escudero Eur. J. Med. Chem. 2013, 66, 258-68.
“In-peptide synthesis of di-oxazolidinone and dehydroamino acid-oxazolidinone motifs as b-turn inducers” R. De Marco, A. Greco, S. Rupiani, A.Tolomelli, C. Tomasini, S. Pieraccini, L. Gentilucci Org. Biomol. Chem. 2013, 11, 4316-4326.
“Molecular Docking of Opiates and Opioid Peptides, a Tool for the Design of Selective Agonists and Antagonists, and for the Investigation of Atypical Ligand-Receptor Interactions”, L. Gentilucci, A. Tolomelli, R. De Marco, R. Artali, Curr. Med. Chem. 2012, 19, 1587-1601.
“Exploring the reactivity of alkylidene malonamides: synthesis of polyfunctionalized isoxazolidinones, aziridines and oxazolines.” A.Tolomelli, G. Cardillo, L. Gentilucci, R. Juris, A. Viola , E. Juaristi, ARKIVOC, 2012, 5, 196-209.
“Opioid Activity Profiles of Oversimplified Peptides Lacking in the Protonable N-Terminus”, R. De Marco, A. Tolomelli, S. Spampinato, A. Bedini, L. Gentilucci, J. Med. Chem. 2012, 55, 10292-10296.
“Expedient synthesis of pseudo-Pro-containing peptides: towards constrained peptidomimetics and foldamers”, R. De Marco, A. Tolomelli, M. Campitiello, P. Rubini, L. Gentilucci, Org. Biomol. Chem. 2012, 10, 2307-2317.
“A straightforward route to enantiopure 2-substituted-3,4-dehydro-b-proline via ring closing metathesis” A. Tolomelli, L. Gentilucci, E. Mosconi, A. Viola, E. Paradisi, AMINO ACIDS 2011, 41, 575-586.
“A novel family of minimalist opioid peptides deprived of the classic pharmacophores” L. Gentilucci, R. De Marco, A. Tolomelli, S. Feddersen, S. Spampinato, A. Bedini, R. Artali PHARMACOLOGICAL REPORTS , 2011, 63, 212-212.
“Development of isoxazoline-containing peptidomimetics as dual a vb 3 and a 5b 1 integrin ligands.” A. Tolomelli, L. Gentilucci, E. Mosconi, A. Viola, S. D. Dattoli, M. Baiula, S. Spampinato, L. Belvisi, M. Civera ChemMedChem, 2011, 6, 2264-2272.
“The Inverse Type II beta-Turn on D-Trp-Phe, a Pharmacophoric Motif for MOR Agonists” L. Gentilucci, A. Tolomelli, R. De Marco ChemMedChem, 2011, 6, 1640-1653.
“Synthesis of Constrained Peptidomimetics Containing 2-Oxo-1,3-oxazolidine-4-carboxylic Acids” L. Gentilucci, A. Tolomelli, R. De Marco, Eur. J. Org. Chem., 2011, 4925-4930.
“Design and Synthesis of Opioid Peptide Analogues and Mimetics”, R. De Marco, L. Gentilucci, A. Tolomelli, Pharm. Reports 2011, 63, 226.
“Antiangiogenic Effect of Dual/Selective a5b1/avb3 Integrin Antagonists Designed on Partially Modified Retro-Inverso Cyclotetrapeptide Mimetics” L. Gentilucci, G. Cardillo, S. Spampinato, A. Tolomelli, F. Squassabia, R. De Marco, A. Bedini, M. Baiula, L. Belvisi, M. Civera, J. Med. Chem. 2010, 53, 106-118.
“Highly regio- and stereoselective palladium-catalyzed allylic carbonate amination. A practical route to dehydro-β-amino esters” G. Cardillo, L. Gentilucci, E. Mosconi, A. Tolomelli, S. Troisi, E. Juaristi Tetrahedron 2010, 66, 4994-4999.
“A simple route towards peptide analogues containing substituted (S)- or (R)-tryptophans” L. Gentilucci, L. Cerisoli, R. De Marco, A. Tolomelli Tetr. Lett. 2010, 51, 2576-2579.
“Synthesis of chiral non-racemic intermediates and Arg-Gly-Asp mimetics by CaLB-catalyzed resolution” G. Cardillo, A. Gennari, L. Gentilucci, E. Mosconi, A. Tolomelli, S. Troisi Tetrahedron: Asymmetry 2010, 21, 96-102.
“Stereoselective Synthesis of Linear and Cyclic Dehydro-b-amino Acids for the Preparation of a vb 3 and a 5b 1 Integrin Inhibitors” G. Cardillo, L. Gentilucci, E.Mosconi, A. Viola, A. Tolomelli, Bol. Soc. Quim. Mex. 2010, 4, 63.
“Determination of the Biologically Active Structure of the Atypical MOR-Ligand c[D-Asp-1-amide-b-Ala-D-Trp-Phe] and Analogues by NMR and Molecular Docking” L. Gentilucci, A. Tolomelli, R. De Marco, S. Spampinato, A. Bedini, R. Artali Bol. Soc. Quim. Mex. 2010, 4, 96.
“Peripheral antinociceptive effects of the cyclic endomorphin-1 analog c[YpwFG] in a mouse visceral pain model” A. Bedini, M. Baiula, L. Gentilucci, A. Tolomelli, R. De Marco, S. Spampinato PEPTIDES 2010, 31 , 2135-2140.
“A convenient synthesis of functionalized isoxazolines and related 5-hydroxyisoxazolidine-4-carboxylates” F. Benfatti, G. Cardillo, S. Contaldi, L. Gentilucci, E. Mosconi, A. Tolomelli, E. Juaristi, G. Reyes-Rangel Tetrahedron, 2009, 65, 2478-2483.
“Synthesis and conformational analysis of cyclotetrapeptide mimetic b-turn templates, and validation as 3D scaffolds.” L. Gentilucci, G. Cardillo, A. Tolomelli, R. De Marco, S. Spampinato, A. Spartà ChemMedChem, 2009, 4, 517-523.
“Dehydro-β-amino acid containing peptides as promising sequences for drug development“ G. Cardillo, A. Gennari, L. Gentilucci, E. Mosconi, A. Tolomelli, S. Troisi Eur. J. Org. Chem. 2009, 34, 5991-5997.
“Asymmetric Synthesis of Three and Four Membered Ring Heterocycles.” (Chapter 1) G. Cardillo, L. Gentilucci, A. Tolomelli in Asymmetric Synthesis of Nitrogen Heterocycles, Jacques Royer Editor, Wiley VCH, 2009.
“Cyclopeptide analogs for generating new molecular and 3D diversity” L. Gentilucci, G. Cardillo, A. Tolomelli, F. Squassabia, R. De Marco, G. Chiriano, Comb. Chem. H. Thr. Scr. 2009, 10, 929-939.
“Cyclotetrapeptide mimics based on a 13-membered, partially modified retro-inverso structure.“ L. Gentilucci, G. Cardillo, A. Tolomelli, S. Spampinato, A. Sparta, F. Squassabia, Eur. J. Org. Chem. 2008, 4, 729-735.
“Investigation of the interaction between the atypical agonist c[YpwFG] and MOR.” Gentilucci, F. Squassabia, R. Demarco, R. Artali, G. Cardillo, A. Tolomelli, S. Spampinato, A. Bedini, FEBS Journal 2008, 275(9), 2315-2337.
“Synthesis of dehydro-β-amino esters via highly regioselective amination of allylic carbonates.” F. Benfatti, G. Cardillo, L. Gentilucci, E. Mosconi, A. Tolomelli, Org. Lett. 2008, 12, 2425-2428.
“Lewis acid induced highly regioselective synthesis of a new class of substituted isoxazolidines “ F. Benfatti, G. Cardillo, L. Gentilucci, E. Mosconi, A. Tolomelli, Synlett 2008, 2605-2608.
“The cycloaddition reaction between α-bromo vinylketenes and imines: a combined experimental and theoretical study.” F. Benfatti, A. Bottoni, G. Cardillo, S. Fabbroni, L. Gentilucci, M. Stenta, A. Tolomelli, Adv Synth. Cat. 2008, 350, 2261-2273.
“Synthesis of Ethyl 5-Hydroxyisoxazolidine-4-carboxylates via Michael Addition/Intramolecular Hemiketalisation” F. Benfatti, A. Bottoni, G. Cardillo, L. Gentilucci, M. Monari, E. Mosconi, M. Stenta , A. Tolomelli Eur. J. Org. Chem. 2008, 36, 6119-6127.
“A Nonclassical Stereoselective Semi-Synthesis of Drospirenone via Cross-Metathesis Reaction” M. Bandini, M. Contento, A. Garelli, M. Monari, A. Tolomelli, A. Umani-Ronchi, E. Andriolo, M. Montorsi Synthesis, 2008, 3801-3804.
“Topological exploration of cyclic endomorphin-1 analogues, structurally defined models for investigating the bioactive conformation of MOR agonists.” L. Gentilucci, A. Tolomelli, F. Squassabia, Protein & Peptide Letters 2007, 14, 51-56.
“Synthesis and biological evaluation of unprecedented classes of spiro-β -lactams and azido-β-lactams as acyl-CoA:cholesterol acyltransferase inhibitors.” F. Benfatti, G. Cardillo, L. Gentilucci, A. Tolomelli, Bioorg. Med. Chem. Lett. 2007, 7, 1946-1950.
“Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics.” L. Gentilucci, G. Cardillo, F. Squassabia, A. Tolomelli, S. Spampinato, A. Sparta, M. Baiula, Bioorg. Med. Chem. Lett. 2007, 8, 2329-2333.
“A microwave-enhanced, Lewis acid-catalyzed synthesis of 1,3-dioxolanes and oxazolines from epoxides.” F. Benfatti, G. Cardillo, L. Gentilucci, A. Tolomelli, M. Monari, F. Piccinelli, Adv. Synt. Cat. 2007, 7, 1256-1264.
“Synthesis of four-membered ring spiro-β -lactams by epoxide ring-opening.” F. Benfatti, G. Cardillo, L. Gentilucci, A. Tolomelli, Eur. J. Org. Chem. 2007, 19, 3199-3205.
“Synthesis and biological evaluation of non-peptide avb 3/a5b 1 integrin dual antagonists containing 5,6-dihydropyridin-2-one scaffolds. “ F. Benfatti, G. Cardillo, S. Fabbroni, P. Galzerano, L. Gentilucci, R. Juris, A. Tolomelli, M. Baiula, A. Sparta, S. Spampinato, Bioorg. Med. Chem. 2007, 15, 7380-7390.
“Enzymatic resolution of ethyl 3-hydroxy-2-(1'-substituted-methylidene)butyrate by Pseudomonas Cepacia lipase catalyzed acetylation.” F. Benfatti, G. Cardillo, L. Gentilucci, E. Mosconi, A. Tolomelli, Tetrahedron: Asymmetry 2007, 18, 2227-2232.
"Synthesis of Enantiomerically pure avb3 integrin ligands based on a 5,6-dihydropyridin-2-one scaffold", F. Benfatti, G. Cardillo, S. Fabbroni, L. Gentilucci, R. Perciaccante, A. Tolomelli, M. Baiula, S. Spampinato, Tetrahedron: Asymm. 2006, 17, 167-170.
"A Novel Family of Minimal PMRI Cyclic Peptides as Versatile Scaffolds for Generating New Molecular Topology", L. Gentilucci, G. Cardillo, A.Tolomelli, F.Squassabia, C. Tiozzo, Med. Chem. 2006, 2, 395-400.
"Theoretical and Experimental Study on the Cycloaddition Reaction between α-Bromo- vinylketenes and imines.", F. Benfatti, A. Bottoni, G. Cardillo, S. Fabbroni, L. Gentilucci, R. Perciaccante, M. Stenta, A. Tolomelli, J. Mex. Chem. Soc. 2006, 50, SI1, 154 (Acts 16th IUPAC ICOS 2006).
"Minimalistic Peptidomimetic Scaffolds Based on the "Partially Modified Retro-Inverso" Peptide Concept", L.Gentilucci, G. Cardillo, A. Tolomelli, F. Squassabia, C. Tiozzo, F. Benfatti. J. Mex. Chem. Soc. 2006, 50, SI1, 204 (Acts 16th IUPAC ICOS 2006).
"Synthesis and Biological Investigation of 5,6-Dihydropyridin-2-one Based RGD Analogues.", F. Benfatti, G. Cardillo, S. Fabbroni, L. Gentilucci, R. Perciaccante, A. Tolomelli, M. Baiula, S. Spampinato, J. Mex. Chem. Soc. 2006, 50, SI1, 204 (Acts 16th IUPAC ICOS 2006).
"Unusual amino acids: synthesis and introduction into naturally occurring peptides and biologically active analogues.", G. Cardillo, L. Gentilucci, A. Tolomelli, Mini Review in Medicinal Chemistry, 2006, 6, 293-304.
“Peptides and peptidomimetics in medicine, surgery and biotechnology.” L. Gentilucci, A. Tolomelli, F. Squassabia, Curr. Med. Chem. 2006, 13, 2449-2466.
“Synthesis and Biological Evaluation of Azido- and Aziridino-hydroxyl-β-lactams through Stereo- and Regioselective Epoxide Ring Opening. “ F. Benfatti, G. Cardillo, L. Gentilucci, R. Perciaccante, A. Tolomelli, A. Catapano, J. Org. Chem. 2006, 71, 9229-9232.
"Zinc metal-promoted nucleophilic addition of azetidin-2-ones to aldehydes and nitriles.", F. Benfatti, G. Cardillo, S. Fabbroni, L. Gentilucci, R. Perciaccante, F. Piccinelli, A. Tolomelli, Synthesis 2005, 61-70.
"Highly Diastereoselective Allylic Azide Formation and Isomerization. Synthesis of 3(2'-Amino)-β-lactams." G. Cardillo, S. Fabbroni, L. Gentilucci, R. Perciaccante, F. Piccinelli, A. Tolomelli, Org. Lett. 2005, 4, 533-536.
"Highly regio- and diastereoselective palladium-catalyzed allylic substitution. Synthesis of 3-(2-aminobutylidene)-4-arylazetidin-2-ones.", G. Cardillo, S. Fabbroni, L. Gentilucci, R. Perciaccante, A. Tolomelli, Adv. Synth. Cat. 2005, 6, 833-838.
"Introduction of hydroxyl- or keto-functionalities into the side chain of azetidin-2-ones via allylic bromide rearrangement, followed by supported reagent substitution.", F. Benfatti, G. Cardillo, S. Fabbroni, L. Gentilucci, R. Perciaccante, A. Tolomelli, ARKIVOC 2005, 6, 136-152.
"An investigation of the reactivity of MCPBA and α-bromoalkenes under traditional or microwave assisted conditions. Selective formation of epoxides or allylic bromides.", F. Benfatti, G. Cardillo, L. Gentilucci, R. Perciaccante, A. Tolomelli, Synlett, 2005, 2204-2208.
“a-Bromo-b,g-unsaturated Ketenes as Valuable Intermediates in the Synthesis of a-amino-b,g-Unsaturated Acids”, G. Cardillo, S. Fabbroni, L. Gentilucci, R. Perciaccante, A. Tolomelli, Tetrahedron: Asymm., 2004, 15, 593-601.
“Recent Advances in the Investigation of the Bioactive Conformation of Peptides Active at the µ-Opioid Receptor. Conformational Analysis of Endomorphins”, L. Gentilucci, A. Tolomelli, Curr. Top. Med. Chem., 2004, 4, 105-121.
“Practical Synthesis of 3-Bromo-5,6-dihydropyridin-2-ones via b,g-unsaturated α-bromo-ketene-imine cycloaddition reaction.”, G. Cardillo, S. Fabbroni, L. Gentilucci, R. Perciaccante, F. Piccinelli, A. Tolomelli, Tetrahedron, 2004, 60, 5031-5040.
"Synthesis and Evaluation of the Affinity toward µ-Opioid Receptors of Atypical, Lipophilic Ligands Based on the Sequence c[-Tyr-Pro-Trp-Phe-Gly-].", G. Cardillo, L. Gentilucci, A. Tolomelli, R. Spinosa, M. Calienni, A. R. Qasem, S. Spampinato, J. Med. Chem. 2004, 47, 5198-5203.
“Stability against enzymatic hydrolysis of endomorphin-1 analogues containing β-proline.”, G. Cardillo, L. Gentilucci, A. Tolomelli, M. Calienni, A. R. Qasem, S. Spampinato, Org. Biomol. Chem., 2003, 1, 1498-1502.
“A straightforward method for the synthesis of alkylidene and arylidene malonates through proline-catalyzed Knoevenagel condensation.”, G. Cardillo, S. Fabbroni, L. Gentilucci, M. Gianotti, A. Tolomelli , Synt. Comm. 2003, 33, 1587-1594.
“Conformational analysis and µ-opioid receptor affinity of short peptides, endomorphin models in a low polarity solvent.”, G. Cardillo, L. Gentilucci, A. Tolomelli, S. Spampinato, M.Calienni, Org. Biomol. Chem. 2003, 1, 3010-3014.
“Aziridines and oxazolines: valuable intermediates in the synthesis of unusual amino acids.”, G. Cardillo, L. Gentilucci, A. Tolomelli, Aldrichimica Acta, 2003, 36, 39-50.
“Antinociception by a peripherally administered novel endomorphin-1 analogue containing D-proline.” S. Spampinato, A. R. Qasem, M. Calienni, G. Murari, L. Gentilucci, A. Tolomelli, G. Cardillo, Eur. J. Pharm., 2003, 469(1-3), 89-95.
“Enantioselective Synthesis of Aziridine 2,2-Dicarboxylates. Copper II-Bisoxazoline Complex Catalysed Michael Reaction on Alkylidene Malonates. (Part I)”, G. Cardillo, S. Fabbroni, L. Gentilucci, M. Gianotti, R. Perciaccante, A. Tolomelli, Tetrahedron: Asymmetry, 2002, 13, 1407-1410.
”Enantioselective Synthesis of Aziridine 2,2-Dicarboxylates. Determination of the Absolute Configuration. (Part II)”, G. Cardillo, S. Fabbroni, L. Gentilucci, M. Gianotti, R. Perciaccante, S. Selva, A.Tolomelli, Tetrahedron: Asymmetry, 2002, 13, 1411-1415.
“NMR Investigations on Boron Complexes in the Conjugate Addition on a,b-Unsaturated Imides”, G. Cardillo, L. Gentilucci, M. Gianotti, A. Tolomelli, Org. Lett., 2001, 3, 1165-1167.
“Microwave-Assisted Ring Expansion of N-Acetyl 3’-Unsubstituted Aziridine in the Presence of Lewis Acids”, G. Cardillo, L. Gentilucci, M. Gianotti, A. Tolomelli, Tetrahedron, 2001, 57, 2807-2812.
“Asymmetry Synthesis of 5-Isopropyl-oxazoline-4-imide as Syn-Hydroxyleucine Precursor”, G. Cardillo, L. Gentilucci, M. Gianotti, A. Tolomelli, Tetrahedron: Asymm., 2001, 12, 563-569.
“Conjugate addition of hydroxylamino derivatives to alkylidene malonates in the presence of chiral Lewis acids.”, G. Cardillo, L. Gentilucci, M. Gianotti, H. Kim, R. Perciaccante, A. Tolomelli, Tetrahedron: Asymmetry, 2001, 12, 2395-2398.
“Synthesis of Aziridine-2,2-dicarboxylates via 1,4-Addition of N,O-(Bistrimethylsilyl)hydroxylamine to a,b-Unsaturated Malonates”, G. Cardillo, L. Gentilucci, M. Gianotti, R. Perciaccante, A. Tolomelli, J. Org. Chem., 2001, 66, 8657-8660.
“ A New Selective Synthesis of the Ile-allo-Thr-Gly Tripeptide Fragment of Lysobactin”, S. Armaroli, G. Cardillo, L. Gentilucci., M. Gianotti, A. Tolomelli, Org. Lett., 2000, 2, 1105-1107.
“Lipase-mediated kinetic resolution of allylic(hydroxymethyl)-methylenecyclopentane building blocks”, G.Laval, G. Cardillo, H. Monti, A. Tolomelli, G. Audran, J.-M. Galano, Tetrahedron: Asymmetry, 2000, 11, 1289-1294.
“Synthesis of the Phenylserine-Leucine Fragment Present in the Antibiotic Lysobactin from an Aziridine-2-imide Precursor”, G. Cardillo, L. Gentilucci, M. Gianotti, A. Tolomelli, Eur. J. Org. Chem., 2000, 2489-2494.
“Influence of Lewis Acids on the Regioselectivity of N-Boc-Aziridine-2-carboxylate Microwave-Asssisted Rearrangement”, G. Cardillo, L. Gentilucci, M. Gianotti, A. Tolomelli, Synlett, 2000, 9, 1309-1311.
“A New Diastereoselective Synthesis of anti a-Alkyl a-Hydroxy b-Amino Acids.” G. Cardillo, A. Tolomelli, C. Tomasini, Eur. J. Org. Chem., 1999, 155-161.
“Synthesis of Optically Pure Threonine Containing Dipeptides by Regio and Stereocontrolled Ring Expansion of Aziridine-2-imide Derivatives.”, G. Cardillo, L. Gentilucci, A. Tolomelli, Chem. Comm., 1999, 167-168.
"Asymmetric 1,4 Addition of Grignard Reagents to Chiral a,b-unsaturated Esters in the presence of Lewis Acids” G. Cardillo, L. Gentilucci, A. Tolomelli, C. Tomasini Tetrahedron, 1999, 55, 6231-6242.
“Asymmetric Synthesis of Syn Hydroxyphenylalanine via Aziridine Ring Expansion to an Oxazoline.”, G. Cardillo, L. Gentilucci, A. Tolomelli, Tetrahedron Letters, 1999, 40, 8261-8264.
“A Practical Method for the Synthesis of β-Amino α-Hydroxy Acids. Synthesis of Enantiomerically Pure Hydroxyaspartic Acid and Isoserine.”, G. Cardillo, L. Gentilucci, A. Tolomelli, C. Tomasini, Synlett, 1999, 11, 1727-1730.
“Dipeptides Containing D-Serine and D-Isoserine From the Same (R)-Aziridine-2-Imide by a Simple Reversal of the Synthetic procedure Steps”, G. Cardillo, L. Gentilucci, A. Tolomelli, Tetrahedron, 1999, 55, 15151-15158.
"Formation of Aziridine-2-Amides through 5-Halo-6-Methyl Perhydropyrimidin-4-ones. A Route to Enantiopure L- and D-Threonine and allo-Threonine", G. Cardillo, L. Gentilucci, A. Tolomelli, C. Tomasini J. Org. Chem., 1998, 63, 3458-3462.
"A Stereoselective Synthesis of (2R,3S)-N-Benzoyl Phenylisoserine Methyl Ester" G. Cardillo, L. Gentilucci, A. Tolomelli, C. Tomasini, J. Org Chem., 1998, 63, 2351-8653.
"Diastereoselective Synthesis of 3'-Unsubstituted N-BOC-Aziridine from Easily Available Chiral a,b-Unsaturated Imide", G. Cardillo, L. Gentilucci, I. Ratera Bastardas, A. Tolomelli, Tetrahedron, 1998, 54, 8217-8222.
"Ring Expansion of N-Acyl Aziridine-2-imides to Oxazoline-4-imides, Useful Precursors of Pure β-Hydroxy α-Aminoacids.", G. Cardillo, L. Gentilucci, A. Tolomelli, C. Tomasini Tetrahedron Letters, 1997, 38, 6953-6956.
"Recent Advances in Functional Group Manipulation", A. Tolomelli, C. Tomasini in Seminars in Organic Synthesis, Acts of XXII Summer School "A.Corbella", Gargnano, June 16th-20th 1997, p.309-390.
"Enzymatic Resolution of α-Alkyl-β-Amino Acids Using Immobilized Penicillin G Acylase", G. Cardillo, A. Tolomelli, C. Tomasini J. Org Chem., 1996, 61, 8651-8654.
"Synthesis of Enantiomerically Pure syn and anti α-Hydroxy-β-Amino Acids through Diastereoselective Hydroxylation of Perhydropyrimidin-4-ones" G. Cardillo, A. Tolomelli, C. Tomasini, Tetrahedron, 1995, 51, 11831-11840.
