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Synthesis Group

Synthesis Group

Publications

- Novel RGD Peptidomimetics Embedding 1,2,3-Triazole as Central Scaffold; Synthesis and av ß3 Integrin Affinity. Ni  M.H., Esposito E., Castorina M. and Dal Pozzo A., Letters in Drug Design and Discovery (2011) 8, 401-405

-Tumor-targeted RGD peptide-camptothecin conjugates.  A. Dal Pozzo, M. Ni, E. Esposito, S. Dallvalle, L. Merlini, C. Pisano, M. Castorina, L. Vesci and S. Penco, Biorg. Med.Chem. 2008, in press

-Novel dual targeting antitumoral conjugates. A. Dal Pozzo, E. Esposito, M. Ni and L. Muzi, Bioconjugate Chem. 2008 in press

-Synthesis and Conformational Studies of Novel, Side-Chain Protected, L-(?Me)Ser
Homopeptides.  F.Formaggio, C.Peggion, C.Toniolo, B-Kaptein,Q.B. Broxterman, M. Ni,
 L.Muzi and A. Dal Pozzo, Understanding biology using peptides,  2007 Volume in press

-Novel tumor-targeted peptide-camptothecin conjugates; synthesis and biological evaluation. A. Dal Pozzo, M. Ni, E. Esposito, S.Penco, C. Pisano, L. Vesci, M. Castorina, F.Bucci et al.  , Peptides 2006 ,  Eds: Rolka K., Rekowski P. Silberring, J. ,2006, p. 170.

-Incorporation of C?-Fuoroalkylamino acids into cyclopeptides: Synthesis of RGD analogues and study of their conformational and biological behaviour. A. Dal Pozzo,
M.H. Ni, L. Muzi, R. De Castiglione, R. Mondelli, S. Mazzini, S. Penco, C. Pisano et al
J. Med.Chem., 2005, 49, 1808.

-Amino acid bromides:  their utilization for difficult couplings in solid-phase peptide synthesis.  M. H. Ni, E. Esposito, B. Kaptein, Q.B. Broxterman and A. Dal Pozzo, Tetrahedron Lett. 2005, 46, 6369. 

-Structure-activity studies of novel conformationally constrained RGD cyclic peptides.  A. Dal Pozzo, M.H. Ni, S. Mazzini and M. Castorina, Peptides:2004, Bridges Between Disciplines , Eds: M. Flegel, M. Fridkin, C. Gilon and J. Slaninova, Kenes Int. 2004, p. 812.

-Synthesis of unusual RGD Cyclic Peptides Incorporating Fluoromethylaminoacids,
as selective inhibitors of ?v?3 Integrin.
A. Dal Pozzo, M.N. Ni and L.Muzi, Peptide Revolution, M. Chorev, T. K. Sawyer Eds., Am. Pept.. Soc., 2003, p.711.

-Facile synthesis of a homopeptide containing seven consecutive sterically hindered residues of C?-methyl-Valine via the azido/bromide method.  A. Dal Pozzo, M.H. Ni, B. Kaptein, Q.B. Broxterman and F. Formaggio,  Peptides 2002, E. Benedetti and C. Pedone Eds., Ziino,Napoli, 2002, p.78.

-Amino acid bromides: their N-protection and use in the synthesis of peptides with extremely difficult sequences. A. Dal Pozzo, M.N. Ni, A. Caporale, R. De Castiglione, B. Kaptein, Q.B. Broxterman and F. Formaggio, J. Org.Chem. 2002, 67, 6372.
-N-Protected amino acid bromides: efficient reagents for incorporation into peptides of extremely hindered ?,?-dialkyl- and ?-fluoroalkyl-amino acids. A. Dal Pozzo, R. Bergonzi and M.H.Ni, Tetrahedron Lett. 2001, 42, 3925.

-Amino acid bromides: a convenient choice for very difficult couplings. A. Dal Pozzo, R. Bergonzi, M.N. Ni and P. Cossettini, Peptides: The wave of the future, M. Lebl, R.A. Houghten Eds., Am.Pept. Soc., 2001, p.93.

-Synthesis and antiaggregatory activity of linear retro-inverso RGD peptides.
A. Dal Pozzo, M Fagnoni, R. Bergonzi, L. Vanini, R. de Castiglione, C. Aglio and S. Colli, J. Peptide Res., 2000, 55, 447.

-Preparation and characterization of poly(ethylene glycol)-crosslinked reacetylated chitosans.  A. Dal Pozzo, L. Vanini, M. Fagnoni, M. Guerrini, A. De Benedittis, R.A.A. Muzzarelli, Carbohydrates Polymers, 2000, 42, 201.

-Synthesis of RGD analogues containing ?-trifluoromethylaspartic acid as potential fibrinogen receptor antagonists.  A. Dal Pozzo, K. Dikovskaya, M. Moroni, M. Fagnoni, L. Vanini, R. Bergonzi, R. de Castiglione, P. Bravo and M. Zanda,  J. Chem. Res. (S)  1999, 468.

-Synthesis of ?-Tfm-amino acids and their incorporation into peptides.  M. Moroni, B. Korsch, A. Dal Pozzo and K. Burger. Proc.Deutsches Peptidsymp., Leipzig, 1999, p. 38.

-Synthesis of RGD analogues containing ?-Tfm-Arginine as potential fibrinogen receptor antagonists. A. Dal Pozzo, L. Muzi, M. Moroni, R.Rondanin, R. de Castiglione, P. Bravo and M. Zanda, Tetrahedron , 1998,54, 6028.

-Percutaneous absorption of parabens from cosmetic formulations. A. Dal Pozzo and N. Pastori, Int. J. Cosm. Sci. 1996, 18, 57.

-Effect of Tripeptide-Copper Complexes with Process of Skin Wound Healing and on Cultured Fibroblasts. F. Buffoni, R. Pino and A. Dal Pozzo, Arch.Int. Pharmac. Ther., 1995, 330, 345.

-Configurationally stable retro-inverso peptides containing a 2-methyl-2-alkyl-  malonyl residue. A. Dal Pozzo and E. Laurita, Proc.23rd Eur. Peptide Symp. , H.L.S. Maia, Escom, Leiden , 1995, p. 714.

-H-Gly-His?(NH-CO)Lys-OH, partially modified retro-inverso analogue of growth factor glycyl-L-histidyl-L-lysine with enhanced enzymatic stability. A. Dal Pozzo, K. Kanai, G. Kereszturi and G. Calabrese, Int. J. Peptide Prot. Res., 1993, 41, 561.

-New highly water-soluble phenytoin prodrugs.  A. Dal Pozzo and M. Acquasaliente,
Int. J. Pharmaceutics, 1992, 81, 263.

-Percutaneous Absorption of Nicotinic Acid Derivatives in vitro. A. Dal Pozzo, G. Donzelli, E. Liggeri and L. Rodriguez, J. Pharm. Sci. , 1991, 80, 54.


-Prediction of skin permeation of highly lipophilic compounds: in vitro model with a modified receptor phase.   A. Dal P ozzo, E. Liggeri, C. Delucca and G. Calabrese,
Int. J. Pharmaceutics, 1991, 70, 219.

-Structure-activity relations. Part 5. Antibacterial activity of a series of substituted
(E)-3-(4-Phenylbenzoyl)-acrylic acids, Chalcones, 2-Hydroxychalcones and ?-Bromochalcones. Addition of Cysteine to substituted 3-Benzoylacrylic acids and related compounds.
  K. Bowden, A. Dal Pozzo and C.K. Duah, J.Chem.Res.(S) 1990,377.


-In vitro model for the evaluation of drug distribution and plasma protein-binding relationship. A. Dal Pozzo, G. Donzelli, L. Rodriguez and A. Tajana, Int.J.Pharmaceutics,
1989, 50, 97.

-New heparin complexes active by intestinal absorption: multiple ion pairs with basic organic compounds. A. Dal Pozzo, M. Acquasaliente, M.R.Geron and G.Andriuoli,
Thrombosis Res. 1989, 119-124.

-New monofunctional derivatives of polyethylene glycols via monotrityl intermediates.  A. Dal Pozzo, A. Vigo and G. Donzelli, Macromol. Chem., 1989, 190, 2457.

-3-Carbonylacrylic Derivatives as Potential Antimicrobial Agents. Correlations between Activity and Reactivity towards Cystein.  A. Dal Pozzo, M. Acquasaliente, G. Donzelli , P. De Maria and C. Vicoli., J. Med. Chem., 1987, 30, 1674.

-In vitro model for drug distribution studies in the presence of albumin. 
A. Dal Pozzo and G. Donzelli, Proc.3rd Eur.Congress of Biopharm.and Pharmacokin, Freiburg, 1987, Vol. II, p.530-536.

-Oligomeric drug carriers. P Ferruti and A. Dal Pozzo, J.Bioact. Compat.Pol.,1987,2,148.

-Synthesis and Antimicrobial Properties of New Aroylacrylic Esters of Polyethylene Glycols. A. Dal Pozzo, M. Acquasaliente, F. Delor and P. Ferruti, Il Farmaco,(Ed. Sci) 1986, 622.

-New Functional Derivatives of Polyethylene Glycols; Betain Esters from Bromoacetate Intermediates. A. Dal Pozzo, G. Donzelli and P. Ferruti, J.Bioactive Compat.Polimers, 1986, 1, 198.

-Synthesis of 4-Oxo-4-(3-Pyridyl)-2-Butenoic Acids and Esters, a New Class of Nicotinoyl Derivatives, using Methylsulfinyl Activating and Leaving group.
A. Dal Pozzo, M. Acquasaliente, M.Buraschi  and B.M. Anderson, Synthesis 1984,11, 926.

-Sulphydryl  Enzyme Inactivation by Nicotynoylacrylates.  B. M.Anderson, C.D. Anderson ,G. Donzelli and A. Dal Pozzo, Biochimica and Biophysica Acta, 1984, 787, 215.


-Comparative binding studies of anticonvulsant drugs to bovine serum albumin.
A. Dal Pozzo, M. Acquasaliente and A. Tajana, Il Farmaco (Ed. Sci.) 1983, 38, 610.

-Selective Enzyme Inactivation by Benzoylacrylic Acid Derivatives. B.M. Anderson, M.L. Tanchoco and A. Dal Pozzo, Biochimica and Biophysica Acta, 1982, 703, 204.

-Biologically active unsaturated ?-lactones.  A. Dal Pozzo and A. Dansi, Boll. Chim.Farm., 1979, 118,239-260.

-?,?-Unsaturated ?-Lactones; Correlations between Lipophilicity and Biological Activity. A.Dal Pozzo, A. Dansi and M. Biassoni, Arzeneimittel-Forschung, 1979, 29. 877.

-Kinetics of base-catalysed condensation of 5-methylfuran-2-(3H)-one with 2-hydroxybenzaldehyde.  I.R. Bellobono, A. Dal Pozzo and M.T.Cataldi, J. Chem.Soc., II, 1976, 1773.

-Unsaturated ?-lactones;  Relationship between their structure and antimicrobial activity.  A. Dal Pozzo, A . Dansi and E. Meneghini, Boll. Chim. Farm., 1974, 113, 280.

-Rapporti tra costituzione ed attività antimicrobica di alcuni ?-lattoni.  A. Dal Pozzo, A. Dansi, V. Mariotti and E. Meneghini,  Boll. Chim. Farm., 1972, 111, 342.

-Das Vorkommen gewisser cyclischer Peptide im Maisquellwasser.  A. Dansi, A. Dal Pozzo, V. Mariotti, B. Bonferoni und M. Piccioni, Die Stärke, 1970, 9, 305.

-Studi analitici di alcune associazioni di comune  uso terapeutico, II; metodi di analisi di miscele di sostanze tranquillanti, analgesiche e anestetiche locali.
A. Dal Pozzo,  Boll. Chim. Farm. , 1969, 108, 230.

-Studi analitici di alcune associazioni di uso terapeutico, I ; metodi di analisi di miscele di sostanze balsamiche.  A. Dal Pozzo, 1969, 108, 47.

-Antimicrobici delle piante.  A. Dansi, L. Ravà e A. Dal Pozzo, Chimica del Farmaco e dei prodotti biologicamente attivi, 1969, 18, 249.

-Solubili di distilleria di diversa provenienza industriale: caratteristiche analitiche degli estratti.  A.Dal Pozzo, A. Dansi, E. Meneghini  e C. Zanini, La Chimica e l’Industria,
1968, 50, 773.

-Cyclic Peptides in Maize Grains. A. Dal  Pozzo  and  A. Dansi, Die Stärke,1968, 3, 94.

-Antimicrobici delle piante, Nota II;  Purificazione delle frazioni attive del sugo di tulipano.  A. Dansi, L.Ravà e A. Dal Pozzo, La ricerca scientifica, 1967, 37, 524.

-Über die Wachstumsfactoren der “Distiller’s dried solubles”. A. Dansi,A. Dal Pozzo,
C. Zanini, E.Meneghini und A. Craveri., Liebigs Ann, Chem., 1966, 226.


-La reazione di Scherer su strato sottile. A. Dal Pozzo, Boll. Chim. Farm  1965, 104, 55.

-Sui fattori sconosciuti di crescita dei “Distiller’s dried solubles”, II; La presenza dell’acido mevalonico nella cosiddetta     Vitamina B13. L. Rotta, A. Dansi, A. Dal Pozzo, C. Zanini and I. Reggianini, Boll. Chim. Farm., 1963, 102, 242.

-Studio preliminare sulle proprietà del fattore di crescita denominato “vitamina B13.
A. Dansi, A. Dal Pozzo, C. Zanini e L. Rotta, La Chimica e l’Industria, 1962, 44, 839.

-Sui fattori sconosciuti di crescita dei Distiller’s dried solubles, I;  Accertamento dell’assenza dell’acido orotico nella vitamina B13. A. Dansi, A. Dal Pozzo, L. Rotta e C. Zanini, Boll.  Chim. Farm. 1962, 101, 880.

-Studio preliminare sui principali componenti dell’olio essenziale di mugo. C. Zanin, A.Dal Pozzo e A. Dansi, Boll. Chim. Farm. 1961, 100, 83.

 


Italian and International Patents

-Nuovi Sali di glicosaminoglicani;  procedimento per la loro preparazione e relative composizioni farmaceutiche.  A. Dal Pozzo, M. Acquasaliente, G. Sportoletti, M. Sarret,
P. Ferruti, F. De Sanctis. Brev. Italiano N. 1231915, 1992.

-Glycyl-Histidyl-Lysine (GHK) derivatives. G. Sportoletti and A. Dal Pozzo
PCT/EP93/02004, 1993.

-Profarmaci idrosolubili di difenilidantoina.  A. Dal Pozzo and M. Acquasaliente,
Brev.Italiano N. 01243197. 1994.

-Cyclopeptides derivatives with anti-integrin activity. A. Dal Pozzo, S. Penco, G. Giannini, O. Tinti, C. Pisano, L. Vesci, M.H. Ni,  PCT  WO 2005/111064 A1, 2005.

-Camptothecin conjugated in position 7 to cyclic peptides as cytostatic agents.
A. Dal Pozzo, S. Penco, L. Merlini, G. Giannini, O. Tinti, C. Pisano, F. Zumino, D. Alloatti,
L. Vesci, S. Dalla valle, M.H. Ni, PCT  WO 2005/111063 A1, 2005.

--7-tButoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists.  A. Dal Pozzo  et al......M.H. Ni,   PCT  WO 2005/110486 A2, 2005.

-Camptothecin derivatives conjugated in position 20 with integrin antagonists.
A. Dal Pozzo et al....M. H. Ni,  PCT  WO 2005/110487 A2. 2005.

-Fluoroalkyl cyclopeptide derivatives having antiintegrin  activity.  A. Dal Pozzo,
G. Giannini, C. Pisano, EP 1 539 803 B1, 2007.

-Novel dual targeting antitumoral conjugates. A. Dal Pozzo, E. Esposito, M.H. Ni,
S. Penco, C. Pisano, M. Castorina, L.Vesci, EP 08156575.6, 2008.