Publications

150.

Synthesis and biological evaluation of new glycoconjugated LDH inhibitors as anticancer agents. D’Andrea F, Vagelli G, Granchi C, Guazzelli L, Tuccinardi T, Poli G, Iacopini D, Minutolo F, Di Bussolo V. Molecules. 2019, 24(19). pii: E3520.


149.

Peptidyl-prolyl isomerases in human pathologies. Tuccinardi T, Rizzolio F. Front Pharmacol. 2019, 10:794.


148.

The influence of Echinacea purpurea leaf microbiota on chicoric acid level. Maggini V, De Leo M, Granchi C, Tuccinardi T, Mengoni A, Gallo ER, Biffi S, Fani R, Pistelli L, Firenzuoli F, Bogani 6. Sci Rep. 2019, 9(1):10897.


147.

Former foodstuff products in Tenebrio molitor rearing: Effects on growth, chemical composition, microbiological load, and antioxidant status. Mancini S, Fratini F, Turchi B, Mattioli S, Dal Bosco A, Tuccinardi T, Nozic S, Paci G. Animals (Basel). 2019, 9(8).pii: E484.


146.

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-5. Mangoni AA, Eynde JJV, Jampilek J, Hadjipavlou-Litina D, Liu H, Reynisson J, Sousa ME, Gomes PAC, Prokai-Tatrai K, Tuccinardi T, Sabatier JM, Luque FJ, Rautio J, Karaman R, Vasconcelos MH, Gemma S, Galdiero S, Hulme C, Collina S, Gütschow M, Kokotos G, Siciliano C, Capasso R, Agrofoglio LA, Ragno R, Muñoz-Torrero D. Molecules. 2019, 24(13). pii: E2415.


145.

N-aryl-N’-ureido-O-sulfamates: Potent and selective inhibitors of the human Carbonic Anhydrase VII isoform with neuropathic pain relieving properties. Bozdag M, Poli G, Angeli A, Lucarini E, Tuccinardi T, Di Cesare Mannelli L, Selleri S, Ghelardini C, Winum JY, Carta F, Supuran CT. Bioorg Chem. 2019, 89:103033.


144.

First-of-its-kind STARD3 Inhibitor: In Silico Identification and Biological Evaluation as Anticancer Agent. Lapillo M, Salis B, Palazzolo S, Poli G, Granchi C, Minutolo F, Rotondo R, Caligiuri I, Canzonieri V, Tuccinardi T, Rizzolio F. ACS Med Chem Lett. 2019, 10(4):475-480.


143.

Virtual screening identifies a PIN1 inhibitor with possible antiovarian cancer effects. Russo Spena C, De Stefano L, Poli G, Granchi C, El Boustani M, Ecca F, Grassi G, Grassi M, Canzonieri V, Giordano A, Tuccinardi T, Caligiuri I, Rizzolio F. J Cell Physiol. 2019, 234(9):15708-15716.


142.

Metalloprotease inhibitor profiles of human ADAM8 in vitro and in cell-based assays. Schlomann U, Dorzweiler K, Nuti E, Tuccinardi T, Rossello A, Bartsch JW. Biol Chem. 2019, 400(6):801-810.


141.

New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents. Chiarelli LR, Mori M, Beretta G, Gelain A, Pini E, Sammartino JC, Stelitano G, Barlocco D, Costantino L, Lapillo M, Poli G, Caligiuri I, Rizzolio F, Bellinzoni M, Tuccinardi T, Villa S, Meneghetti F. J Enzyme Inhib Med Chem. 2019,34(1):823-828.


140.

Novel 8-substituted coumarins that selectively inhibit human carbonic anhydrase IX and XII. Buran K, Bua S, Poli G, Önen Bayram FE, Tuccinardi T, Supuran CT. Int J Mol Sci. 2019, 20(5). pii: E1208.


139.

Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines. Krasavin M, Shetnev A, Baykov S, Kalinin S, Nocentini A, Sharoyko V, Poli G, Tuccinardi T, Korsakov M, Tennikova TB, Supuran CT. Eur J Med Chem. 2019, 168:301-314.


138.

Extensive Reliability Evaluation of Docking-Based Target-Fishing Strategies. Lapillo M, Tuccinardi T, Martinelli A, Macchia M, Giordano A, Poli G. Int J Mol Sci. 2019, 20(5). pii: E1023.


137.

Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor. Granchi C, Lapillo M, Glasmacher S, Bononi G, Licari C, Poli G, El Boustani M, Caligiuri I, Rizzolio F, Gertsch J, Macchia M, Minutolo F, Tuccinardi T, Chicca A. J Med Chem. 2019, 62(4):1932-1958.


136.

The acyl-glucuronide metabolite of ibuprofen has analgesic and anti-inflammatory effects via the TRPA1 channel. De Logu F, Li Puma S, Landini L, Tuccinardi T, Poli G, Preti D, De Siena G, Patacchini R, Tsagareli MG, Geppetti P, Nassini R. Pharmacol Res. 2019, 142:127-139.


135.

Computationally driven discovery of phenyl(piperazin-1-yl)methanone derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors. Poli G, Lapillo M, Jha V, Mouawad N, Caligiuri I, Macchia M, Minutolo F, Rizzolio F, Tuccinardi T, Granchi C. J Enzyme Inhib Med Chem. 2019, 34(1):589-596.


134.

A Guide to PIN1 Function and Mutations Across Cancers. El Boustani M, De Stefano L, Caligiuri I, Mouawad N, Granchi C, Canzonieri V, Tuccinardi T, Giordano A, Rizzolio F. Front Pharmacol. 2019, 9:1477.


133.

Identification of the First Synthetic Allosteric Modulator of the CB 2 Receptors and Evidence of Its Efficacy for Neuropathic Pain Relief. Gado F, Di Cesare Mannelli L, Lucarini E, Bertini S, Cappelli E, Digiacomo M, Stevenson LA, Macchia M, Tuccinardi T, Ghelardini C, Pertwee RG, Manera C. J Med Chem. 2019, 62(1):276-287.


132.

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes⁻4. Mangoni AA, Guillou C, Vanden Eynde JJ, Hulme C, Jampilek J, Li W, Prokai-Tatrai K, Rautio J, Collina S, Tuccinardi T, Sousa ME, Sabatier JM, Galdiero S, Karaman R, Kokotos G, Torri G, Luque FJ, Vasconcelos MH, Hadjipavlou-Litina D, Siciliano C, Gütschow M, Ragno R, Gomes PAC, Agrofoglio LA, Muñoz-Torrero D. Molecules. 2019, 24(1). pii: E130.


131.

Continued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: Discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively kill cancer cells in hypoxic environment. Krasavin M, Shetnev A, Sharonova T, Baykov S, Kalinin S, Nocentini A, Sharoyko V, Poli G, Tuccinardi T, Presnukhina S, Tennikova TB, Supuran CT. Eur J Med Chem. 2019, 164:92-105.


130.

Design, synthesis and biological evaluation of bifunctional inhibitors of membrane type 1 matrix metalloproteinase (MT1-MMP). Cuffaro D, Nuti E, Gifford V, Ito N, Camodeca C, Tuccinardi T, Nencetti S, Orlandini E, Itoh Y, Rossello A. Bioorg Med Chem. 2019, 27(1):196-207.


129.

Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors. Bononi G, Granchi C, Lapillo M, Giannotti M, Nieri D, Fortunato S, Boustani ME, Caligiuri I, Poli G, Carlson KE, Kim SH, Macchia M, Martinelli A, Rizzolio F, Chicca A, Katzenellenbogen JA, Minutolo F, Tuccinardi T. Eur J Med Chem. 2018, 157:817-836.


128.

Development of a Fingerprint-Based Scoring Function for the Prediction of the Binding Mode of Carbonic Anhydrase II Inhibitors. Poli G, Jha V, Martinelli A, Supuran CT, Tuccinardi T. Int J Mol Sci. 2018, 19(7). pii: E1851.


127.

Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes-3. Mangoni AA, Tuccinardi T, Collina S, Vanden Eynde JJ, Muñoz-Torrero D, Karaman R, Siciliano C, de Sousa ME, Prokai-Tatrai K, Rautio J, Guillou C, Gütschow M, Galdiero S, Liu H, Agrofoglio LA, Sabatier JM, Hulme C, Kokotos G, You Q, Gomes PAC. Molecules. 2018, 23(7). pii: E1596.


126.

Discovery and development of novel salicylate synthase (MbtI) furanic inhibitors as antitubercular agents. Chiarelli LR, Mori M, Barlocco D, Beretta G, Gelain A, Pini E, Porcino M, Mori G, Stelitano G, Costantino L, Lapillo M, Bonanni D, Poli G, Tuccinardi T, Villa S, Meneghetti F. Eur J Med Chem. 2018, 155:754-763.


125.

New Chromane-Based Derivatives as Inhibitors of Mycobacterium tuberculosis Salicylate Synthase (MbtI): Preliminary Biological Evaluation and Molecular Modeling Studies. Pini E, Poli G, Tuccinardi T, Chiarelli LR, Mori M, Gelain A, Costantino L, Villa S, Meneghetti F, Barlocco D. Molecules. 2018, 23(7). pii: E1506.


124.

Identification of Lactate Dehydrogenase 5 Inhibitors using Pharmacophore- Driven Consensus Docking. Poli G, Scarpino A, Aissaoui M, Granchi C, Minutolo F, Martinelli, Tuccinardi T. Curr Bioact Comp. 2018, 14:197-204.


123.

Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system. Chicca A, Arena C, Bertini S, Gado F, Ciaglia E, Abate M, Digiacomo M, Lapillo M, Poli G, Bifulco M, Macchia M, Tuccinardi T, Gertsch J, Manera C. Eur J Med Chem. 2018, 154:155-171.


122.

Anticancer Activity of Euplotin C, Isolated from the Marine Ciliate Euplotes crassus, Against Human Melanoma Cells. Carpi S, Polini B, Poli G, Alcantara Barata G, Fogli S, Romanini A, Tuccinardi T, Guella G, Frontini FP, Nieri P, Di Giuseppe G. Mar Drugs. 2018, 16(5). pii: E166.


121.

Liposomal delivery of a Pin1 inhibitor complexed with cyclodextrins as new therapy for high-grade serous ovarian cancer. Spena CR, De Stefano L, Palazzolo S, Salis B, Granchi C, Minutolo F, Tuccinardi T, Fratamico R, Crotti S, D’Aronco S, Agostini M, Corona G, Caligiuri I, Canzonieri V, Rizzolio F. J Control Release. 2018, 281:1-10.


120.

Binding investigation and preliminary optimisation of the 3-amino-1,2,4-triazin-5(2H)-one core for the development of new Fyn inhibitors. Poli G, Lapillo M, Granchi C, Caciolla J, Mouawad N, Caligiuri I, Rizzolio F, Langer T, Minutolo F, Tuccinardi T. J Enzyme Inhib Med Chem. 2018, 33(1):956-961.


119.

Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors. Aghazadeh Tabrizi M, Baraldi PG, Baraldi S, Ruggiero E, De Stefano L, Rizzolio F, Di Cesare Mannelli L, Ghelardini C, Chicca A, Lapillo M, Gertsch J, Manera C, Macchia M, Martinelli A, Granchi C, Minutolo F, Tuccinardi T. J Med Chem. 2018, 61(3):1340-1354.


118.

Heterocyclic periphery in the design of carbonic anhydrase inhibitors: 1,2,4-Oxadiazol-5-yl benzenesulfonamides as potent and selective inhibitors of cytosolic hCA II and membrane-bound hCA IX isoforms. Krasavin M, Shetnev A, Sharonova T, Baykov S, Tuccinardi T, Kalinin S, Angeli A, Supuran CT. Bioorg Chem. 2018, 76:88-97.


117.

Three-Dimensional Analysis of the Interactions between hLDH5 and Its Inhibitors. Poli G, Granchi C, Aissaoui M, Minutolo F, Tuccinardi T. Molecules. 2017, 22(12):2217.


116.

A patent review of Monoacylglycerol Lipase (MAGL) inhibitors (2013-2017). Granchi C, Caligiuri I, Minutolo F, Rizzolio F, Tuccinardi T. Expert Opin Ther Pat. 2017, 27(12):1341-1351.


115.

Lucky switcheroo: dramatic potency and selectivity improvement of imidazoline inhibitors of human carbonic anhydrase VII. Kalinin S, Kopylov S, Tuccinardi T, Sapegin A, Darin D, Angeli A, Supuran CT, Krasavin M. ACS Med Chem Lett. 2017, 8(10):1105-1109.


114.

Development of terphenyl-2-methyloxazol-5(4H)-one derivatives as selective reversible MAGL inhibitors. Granchi C, Caligiuri I, Bertelli E, Poli G, Rizzolio F, Macchia M, Martinelli A, Minutolo F, Tuccinardi T. J Enzyme Inhib Med Chem. 2017, 32(1):1240-1252.


113.

Constituents of Polygala flavescens ssp. flavescens and Their Activity as Inhibitors of Human Lactate Dehydrogenase. De Leo M, Peruzzi L, Granchi C, Tuccinardi T, Minutolo F, De Tommasi N, Braca A. J Nat Prod. 2017, 80(7):2077-2087.


112.

Characterization of the Saffron Derivative Crocetin as an Inhibitor of Human Lactate Dehydrogenase 5 in the Antiglycolytic Approach against Cancer. Granchi C, Fortunato S, Meini S, Rizzolio F, Caligiuri I, Tuccinardi T, Lee HY, Hergenrother PJ, Minutolo F. J Agric Food Chem. 2017, 65(28):5639-5649.


111.

Primary mono- and bis-sulfonamides obtained via regiospecific sulfochlorination of N-arylpyrazoles: inhibition profile against a panel of human carbonic anhydrases. Krasavin M, Korsakov M, Ronzhina O, Tuccinardi T, Kalinin S, Tanç M, Supuran CT. J Enzyme Inhib Med Chem. 2017, 32(1):920-934.


110.

Bifunctional Inhibitors as a new tool to reduce cancer cell invasion by impairing MMP-9 homodimerization. Nuti E, Rosalia L, Cuffaro D, Camodeca C, Giacomelli C, Da Pozzo E, Tuccinardi T, Costa C, Antoni C, Vera L, Ciccone L, Orlandini E, Nencetti E, Dive V, Martini C, Stura EA, Rossello A. ACS Med Chem Lett. 2017, 8(3):293-298.


109.

Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3- and 4-(hetero)arylisoxazol-5-amine scaffolds. Krasavin M, Korsakov M, Zvonaryova Z, Semyonychev E, Tuccinardi T, Kalinin S, Tanç M, Supuran CT. Bioorg. Med. Chem. 2017, 25(6):1914-1925.


108.

Antibacterial and Hypoglycemic Diterpenoids from Salvia chamaedryoides. Bisio A, De Mieri M, Milella L, Schito AM, Parricchi A, Russo D, Alfei S, Lapillo M, Tuccinardi T, Hamburger M, De Tommasi N. J. Nat. Prod. 2017, 80(2):503-514.


107.

Immunomodulatory Properties of 1,2-Dihydro-4-hydroxy-2-oxo-1,8-naphthyridine-3-carboxamide Derivative VL15. Malfitano AM, Laezza C, Bertini S, Marasco D, Tuccinardi T, Bifulco M, Manera C. Biochimie. 2017, 135:173-180.


106.

Bottom-Up Synthesis of Carbon Nanoparticles with Higher Doxorubicin Efficacy. Bayda S, Hadla M, Palazzolo S, Kumar V, Caligiuri I, Ambrosi E, Pontoglio E, Agostini M, Tuccinardi T, Benedetti A, Riello P, Canzonieri V, Corona G, Toffoli G, Rizzolio F. J Contr. Rel. 2017, 248:144-152.


105.

Reliability analysis and optimization of the consensus docking approach for the development of virtual screening studies. Poli G, Martinelli Tuccinardi T. J Enzyme Inhib Med Chem. 2016, 31(sup2):167-173.


104.

Structural optimization of 4-chlorobenzoylpiperidine derivatives for the development of potent, reversible and selective monoacylglycerol lipase (MAGL) inhibitors. Granchi C, Rizzolio F, Palazzolo S, Carmignani S, Macchia M, Saccomanni G, Manera C, Martinelli A, Minutolo F, Tuccinardi T. J Med Chem. 2016, 59(22):10299-10314.


103.

Drug affinity responsive target stability (DARTS) identifies laurifolioside as a new clathrin heavy chain modulator. Dal Piaz F, Saltos MBV, Franceschelli S, Forte G, Marzocco S, Tuccinardi T, Poli G, Ebrahimi SN, Hamburger M, De Tommasi N, Braca A. J Nat Prod. 2016, 79(10):2681-2692.


102.

Identification of a new STAT3 dimerization inhibitor through a pharmacophore-based virtual screening approach. Poli G, Gelain A, Porta F, Asai A, Martinelli A, Tuccinardi T. J Enzyme Inhib Med Chem. 2016, 31(6):1011-1017.


101.

Inhibition of carbonic anhydrase isoforms I, II, IX and XII with secondary sulfonamides incorporating benzothiazole scaffolds. Petrou A, Geronikaki A, Terzi E, Ozensoy Guler O, Tuccinardi T, Supuran CT. J Enzyme Inhib Med Chem. 2016, 31(6):1306-1311.


I commenti sono chiusi.