REFERENCES
1. G. Vlahovic, J. Crawford, “Activation of Tyrosine Kinases in Cancer”, The Oncologist 2003, 8, 531-538.
2. P. Blume-Jensen, T. Hunter “Oncogenic kinase signalling” Nature 2001, 411, 355-365.
3. G.M. Pontieri, M. A. Russo, L. Frati, Chapter 22, “Oncogeni”: 585-616, Patologia Generale 2008, 3th Edition., PICCIN.
4. K. Tamura, M. Fukuoka, “Molecular target-based cancer therapy: tyrosine kinase inhibitors”, International Journal of Clinical Oncology 2003, 8, 207- 211.
5. L.M. Ellis, “Epidermal growth factor receptor in tumor angiogenesis”, Hematology/Oncology Clinics of North America 2004, 18, 1007-1021.
6. S. Sebastian, J. Settleman, S.J. Reshkin, A. Azzariti, A. Bellizzi, A. Paradiso,
“The complexity of targeting EGFR signalling in cancer: From expression to turnover”, Biochimica et Biophysica Acta 2006, 1766, 120-139
7. C. Boccaccio, P.M. Comoglio, “The HGF receptor family: unconventional signal transducers for invasive cell growth”, Genes To Cell 1996, 1, 347-354.
8. M.A. Lemmon, “Ligand-induced ErbB receptor dimerization”, Experimental Cell Reserch 2009, 315, 638-648.
9. R. Bianco, T. Gelardi, V. Damiano, F. Ciardiello, G. Tortora, “Rational bases for the development of EGFR inhibitors for cancer treatment”, The International Journal of Biochemistry & Cell Biology 2007, 39, 1416-1431.
10. R. Pérez-Soler, “HER1/EGFR Targeting: Refining the Strategy”, The Oncologist 2004, 9, 58-67.
11. M. Alimandi, A. Cama , R. Mariani-Costantini, L. Frati, “Oncogeni e fattori di crescita tirosinchinasici”, Il Cancro: ricerca e applicazioni cliniche, CNR, Le Scienze 1994, 41-48.
12. B.P. Ceresa, S.L. Schmid, “Regulation of signal transduction by endocytosis”, Current Opinion in Cell Biology 2000, 12, 204-210.
13. G. Carpenter, S. Cohen, “Epidermal growth factor”, Annual Review of Biochemistry 1979, 48, 193-216.
14. A. Vulpetti, R. Bosotti, Sequence and structural analysis of kinase ATP pocket residues, Il Farmaco, 2004, 59, 759-765.
15. S. Trumpp-Kallmeyer, J. R. Rubin, C. Humblet, J.M. Hamby, H.D.H.
Showalter, “Development of Binding Model to Protein Tyrosine Kinases for Substituted Pyrido[2,3-d]pyrimidine Inhibitors”, Journal of Medicinal Chemistry, 1998, 41, 1752-1763.
16. Kerbel, R.S. Carcinogenesis, 2000, 21, 501.
17. B.D. Palmer, S. Trumpp-Kallmeyer, D.W. Fry, J.M. Nelson, H.D.H.
Showalter, W.A. Denny, Tyrosine kinase inhibitors.11. Soluble Analogues of Pyrrolo and Pyrazoloquinazolines as Epidermal Growth Factor Receptor Inhibitors: Synthesis, Biological Evaluation and Modeling of the mode of binding, Journal of Medicinal Chemistry, 1997, 40, 1519-1529.
18. J. Baselga, “Epidermal growth factor receptor pathway inhibitors”, Update on Cancer Therapeutics 2006, I, 299-310.
19. Y. Graziani, E. Erikson, R. Erikson, “The effect of quercetin on the phosphorylation activity of the Rous sarcoma virus transforming gene product in vitro and in vivo”, European Journal of Biochemistry 1983, 135, 583-589.
20. T. Akiyama, J. Ishida, S. Nakagawa, H. Ogawara, S. Watanabe, N. Itoh, M.
Shibuya, Y. Fukami, “Genistein, a Specific Inhibitor of Tyrosine-specific Protein Kinases”, The Journal of Biological Chemistry 1987, 262, 5592-5595.
21. D.W. Fry, A.J. Kraker, A. McMichael, L.A. Ambroso, J.M. Nelson, W.R.
Leopold, R.W. Connors, A.J. Bridges, “A specific inhibitor of the epidermal growth factor receptor tyrosine kinase”, Science 1994, 265, 1093-1095.
22. A. J Barker, K.H. Gibson, W. Grundy, A.A. Godfrey, J.J. Barlow, M.P. Healy, J.R. Woodburn, S.E. Ashton, B.J. Curry, S. Lynn, L. Henthorn, L. Richards,
“Studies Leading to the Identification of ZD1839 (IressaTM): An Orally Active, Selective Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Targeted to the Treatment of Cancer”, Bioorganic & Medicinal Chemistry Letters 2001, 11, 1911–1914.
23. R.S. Herbst, “Targeting the epidermal growth factor receptor in cancer therapy”, Expert Opinion on Investigational Drugs 2002, 11, 837-849.
24. G. Scagliotti, R. Govindan “Targeting Angiogenesis with Multitargeted Tyrosine Kinase Inhibitors in the Treatment of Non-Small Cell Lung Cancer”
Oncologist 2010, 15, 436-446
25. M.L. Janmaat, G. Giaccone, “Small-Molecule Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors”, The Oncologist 2003, 8, 576-586.
26. R.L. Comis, “The Current Situation: Erlotinib (Tarceva®) and Gefitinib (Iressa®) in Non-Small Cell Lung Cancer”, The Oncologist 2005, 10, 467-470.
27. D.W. Rusnak, K. Lackey, K. Afflek, E.R. Wood, K.J. Alligood, N. Rhodes, B.
Keith, D.M. Murray, R.J. Mullin, W.B. Knight, T.M. Gilmer, “The Effects of the Novel Reversible Epidermal Growth Factor Receptor/ErbB-2 Tyrosine Kinase Inhibitor GW572016, on the Growth of Human Normal and Tumor derived Cell Lines in Vitro and in Vivo”, Molecular Cancer Therapeutics 2001, 1, 85.
28. J.B. Smaill, G.W. Rewcastle, J.A. Loo, K.D. Greis, O.H. Chan, E.L. Reyner, E. Lipka, H.D. Showalter, P.W. Vincent, W.L. Elliott, W.A. Denny, “Tyrosine Kinase Inhibitors. Irreversible Inhibitors of the Epidermal Growth Factor Receptor: 4-(Phenylamino)-quinazoline and 4-(Phenylamino)pyrido[3,2- d]pyrimidine-6-acrylamides Bearing Additional Solubilizing Functions”, Journal of Medicinal Chemistry 2000, 43, 1380-1397.
29. S. Klein, A. Levitzki, “Targeting the EGFR and the PKB pathway in cancer”, Current Opinion in Cell Biology 2009, 21, 185–193.
30. O. Dassonville, A. Bozec, J.L. Fischel, G. Milano, “EGFR Targeting Therapies: Monoclonal antibodies versus tyrosine kinase inhibitors.
Similarities and differences”, Clical reviews in Oncology/Hematology 2007, 62, 53-61
31. N. Ferrara, “Role of vascular endothelial growth factor in regulation of physiological angiogenesis”, Am. J. Physiol. Cell Physiol. 2001, 280, 1358- 1366.
32. Rosen, L.S. Cancer Control., 2002, 9, 36.
34. Leung, D.W.; Cachianes, D.; Kuang, W.J.; Goeddel, D.V.; Ferrara, N.
Science,1989, 246, 1306.
35. Shibuya, M.; Yamaguchi, S.; Yamane, A.; Ikeda, T.; Tojo, A.; Matsushime, H.; Sato, M. Oncogene, 1990, 5, 519.
36. Matthews, W.; Jordan, C.T.; Gavin, M.; Jenkins, N.A.; Copeland, N.G.;
Lemischka, I.R. Proc. Natl. Acad. Sci. USA, 1991, 88, 9026.
37. Paavonen, K.; Puolakkainen, P.; Jussila, L.; Jahkola, T.; Alitalo, K. Am. J.
Pathol., 2000, 156, 1499.
38. G.D. Yancopoulos, S. Davis, N.W. Gale, J.S. Rudge, S.J. Wiegand, J. Holash,
“Vascular-specific growth factors and blood vessel formation”, Nature 2000, 407, 242-248.
39. C. Wheeler, T. Stephens, K Byth, T. Green, S. Wedge, D. Blakey, A. Hughes,
“Novel approaches in oncology at AstraZeneca”, EJC Supplements 2003, 1, 3- 8.
40. B. Frederick, D. Gustafson, C. Bianco, F. Ciardiello, I. Dimery, D. Raben
“ZD6474, An inhibitor of VEGFR and EGFR tyrosine kinase activity in combination with radiotherapy”, International Journal of Radiation Oncology- Biology-Physics 2006, 64, 33–37.
41. A. Vulpetti, R. Bosotti, Sequence and structural analysis of kinase ATP pocket residues, Il Farmaco, 2004, 59, 759-765.
42. Hanahan, D.; Folkman, J. Cell, 1996, 86, 353.
43. Rahimi, N. Front. Biosci., 2006, 11, 818.
44. Jain, R.K. Nat. Med., 2001, 7, 987.
45. Gasparrini, G. Drugs, 1999, 58, 17.
46. Carmeliet, P.; Moons, L.; Luttun, A.; Vincenti, V.; Compernolle, V.; DeMol, M.; Wu, Y.; Bono, F.; Devy, L.; Beck, H.; Scholz, D.; Acker, T.; Di Palma, T.; Dewerchin, M.; Noel, A.; Stalmans, I.; Barra, A.; Blacher, S.;
Vandendriessche, T.; Ponten, A.; Eriksson, U.; Plate, K.H.; Foidart, J.M.;
Schaper, W.; Charnock-Jones, D.S.; Hicklin, D.J.; Herbert, J.M.; Collen, D.;
Persico, M.G. Nat. Med., 2001, 7, 575.
47. Zhao, Q.; Egashira, K.; Hiasa, K.; Ishibashi, M.; Inoue, S.; Ohtani, K.; Tan, C.; Shibuya, M.; Takeshita, A.; Sunagawa, K. Arterioscler. Thromb. Vasc.
Biol., 2004, 24, 2284.
48. Manley, P.W.; Bold, G.; Bruggen, J.; Fendrich, G.; Furet, P.; Mestan, J.;
Schnell, C.; Stolz, B.; Meyer, T.; Meyhack, B.; Stark, W.; Strauss, A.; Wood, J. Biochim. Biophys. Acta, 2004, 1697, 17.
49. Ferrara, N. Oncology, 2005, 69, 11.
50. Ferrara, N.; Hillan, K.J.; Novotny, W. Biochem. Biophys. Res. Commun., 2005, 333, 328.
51. Ferrara, N.; Damico, L.; Shams, N.; Lowman, H.; Kim, R. Retina, 2006, 26, 859.
52. Lee, J.H.; Canny, M.D.; De Erkenez, A.; Krilleke, D.; Ng, Y.S.; Shima, D.T.;
Pardi, A.; Jucker, F. Proc. Natl. Acad. Sci. USA, 2005, 102, 18902.
53. Weng, D.E.; Usman, N. Curr. Oncol. Rep., 2001, 3, 141.
54. Weng, D.E.; Masci, P.A.; Radka, S.F.; Jackson, T.E.; Weiss, P.A.; Ganapathi, R.; Elson, P.J.; Capra, W.; Parker, V.P.; Lockridge, J.A.; Cowens, J.W.;
Usman, N.; Borden, E.C. Mol. Cancer Ther., 2005, 4, 948.
55. Konner, J.; Dupont, J. Clin. Colorectal Cancer, 2004, (Suppl 2), S81.
56. Nguyen, Q.D.; Shah, S.M.; Hafiz, G.; Quinlan, E.; Sung, J.; Chu, K.;
Cedarbaum, J.M.; Campochiaro, P.A. Ophthalmology, 2006, 113, 1522.
57. T.L. Underiner, B. Ruggeri and D.E. Gingrich, “Development of Vascular Endothelial Growth Factor Receptor (VEGFR) Kinase Inhibitors as Anti- Angiogenic Agents in Cancer Therapy”, Current Medicinal Chemistry, 2004, 11, 731-745.
58. G. Bold et al. “New Anilino Phthalazines as Potent and Orally Well Absorbed Inhibitors of the VEGF Receptor Tyrosine Kinase Useful as Antagonists of Tumor-Driven angiogenesis” Journal of Medicinal Chemistry 2000, 43, 2310- 2323
59. C. Wheeler, T. Stephens, K Byth, T. Green, S. Wedge, D. Blakey, A. Hughes,
“Novel approaches in oncology at AstraZeneca”, EJC Supplements 2003, 1, 3- 8.
60. S. Schenone, F. Bondavalli, M. Botta, “Antiangiogenic agents: an update on small molecule VEGFR inhibitors”, Current Medicinal Chemistry, 2007, 14, 2495-2516.
61. G. Kesisis, H. Broxterman, G. Giaccone, Curr. Pharm. Des., 2007, 13, 2795- 2809.
62. H. Zhong, J.P. Bowen, Curr. Top. Med. Chem., 2007, 7, 1379-1393.
63. A. Kiselyov, K.V. Balakin, S.E. Tkachenko, Expert Opin. Invest. Drugs, 2007, 16, 83-107.
64. G. Bold, K.H. Altmann, J. Frei, M. Lang, P.W. Manley, P. Traxler, B.
Wietfeld, J. Brüggen, E. Buchdunger, R. Cozens, S. Ferrari, , F. Hofmann, G.
Martiny-Baron, J. Mestan, J. Rösel, M. Sills, D. Stover, F. Acemoglu, E. Boss, R. Emmenegger, L. Lässer, E. Masso, R. Roth, C. Schlachter, W. Vetterli, D.
Wyss, J.M: Wood, Journal of Medicinal Chemistry, 2000, 43, 2310-2323.
65. P.W. Manley, P. Furet, G. Bold, J. Brüggen, J. Mestan, T. Meyer, C.R.
Schnell, J. Wood, M. Habery, A. Huth, M. Krüger, A. Menrad, E. Ottow, D.
Seidelmann, G. Siemeister, K.H. Thierauch, Journal of Medicinal Chemistry, 2002, 45, 5687-5693.
66. P.W. Manley, G. Bold, J. Brüggen, G.Fendrich, P. Furet, J. Mestan, C.
Schnell, B. Stolz, T. Meyer, B. Meyhack, W. Stark, A. Strauss, J. Wood, Biochim. Biophys. Acta Proteins Proteomics, 2004, 1697, 17-27.
67. Huse, M.; Kuriyan, J. Cell, 2002, 109, 275.
68. A. Papakyriakou, M.E. Katsarou, M. Belimezi, M. Karpusas, D. Vourloumis,
“Discovery of Potent Vascular Endothelial Growth Factor Receptor-2 Inhibitors”, ChemMedChem, 2010, 5, 118-129.
69. Bold, G.; Furet, P.; Manley, P.W. WO200452884, 2004.
70. Dumas, J.; Dixon, J.A. Exp. Opin. Ther. Patents, 2005, 15, 647.
71. Traxler, P.; Allegrini, P.R.; Brandt, B.; Brueggen, J.; Cozens, R.; Fabbro, D.;
Grosios, K.; Lane, H.A.; McSheehy, P.; Mestan, J.; Meyer, T.; Tang, C.;
Wartmann, M.; Wood, J.; Caravatti, G. Cancer Res., 2004, 64, 4931.
72. Fraley, M.E.; Rubino, R.S.; Hoffmann, W.F.; Hambaugh, S.R.; Arrington, K.L.; Hungate, R.W.; Bilodeau, M.T.; Tebben, A.J.; Bilodeau, M.T.; Tebben,
A.J.; Rutledge, R.Z.; Kendall, R.L.; McFall, R.C.; Huckle, W.R.; Coll, K.E.;
Thomas, K.A. Bioorg. Med. Chem. Lett., 2002, 12, 3537.
73. Munchhof, M.J.; Beebe, J.S.; Casavant, J.M.; Cooper, B.A.; Doty. J.L.;
Higdon, R.C.; Hillermann, S.R.; Soderstrom, C.I.; Knauth, E.A.; Marx, M.A.;
Rossi, A.M.; Sobolov, S.B.; Sun, J. Bioorg. Med. Chem. Lett., 2004, 14, 21.
74. Gangjee, A.; Zeng, Y.; Ihnat, M.; Warnke, L.A.; Green, D.W.; Kisliuk, R.L.;
Lin, F. Bioorg. Med. Chem., 2005, 13, 5475.
75. McDermott, L.A.; Simcox, M.; Higgins, B.; Nevins, T.; Kolinsky, K.; Smith, M.; Yang, H. Li, J.K.; Chen, Y.; Ke, J.; Mallalieu, N.; Egan, T.; Kolis, S.;
Railkar, A.; Gerber, L.; Luk, K.C. Bioorg. Med. Chem., 2005, 13, 4835.
76. McDermott, L.A.; Higgins, B.; Simcox, M.; Luk, K.C.; Nevins, T.; Kolinsky, K.; Smith, M.; Yang, H.; Li, J.K.; Chen, Y.; Ke, J.; Mallalieu, N.; Egan, T.;
Kolis, S.; Railkar, A.; Gerber, L.; Liu, J.J.; Konzelmann, F.; Zhang, Z.; Flynn, T.; Morales, O.; Chen, Y. Bioorg. Med. Chem. Lett., 2006, 16, 1950.
77. Guo, X.N.; Zhong, L.; Tan, J.Z.; Li, J.; Luo, X.M.; Jiang, H.L.; Nan, F.J.; Lin, L.P.; Zhang, X.W.; Ding, J. Cancer Biol. Ther., 2005, 4, 1125.
78. Huang, S.; Li, R.; Connolly, P.J.; Xu, G.; Gaul, M.D.; Emanuel, S.L.;
Lamontagne, K.R.; Greenberger, L.M. Bioorg. Med. Chem. Lett., 2006, 16, 6063.
79. Manley, P.J.; Balitza, A.E.; Bilodeau, M.T.; Coll, K.E.; Hartman, G.D.;
McFall, R.C.; Rickert, K.W.; Rodman, L.D.; Thomas, K.A. Bioorg. Med.
Chem. Lett., 2003, 13, 1673.
80. Emanuel, S.; Gruninger, R.H.; Fuentes-Pesquera, A.; Connolly, P.J.; Seamon, J.A.; Hazel, S.; Tominovich, R.; Hollister, B.; Napier, C.; D'Andrea, M.R.;
Reuman, M.; Bignan, G.; Tuman, R.; Johnson, D.; Moffatt, D.; Batchelor, M.;
Foley, A.; O'Connell, J.; Allen, R.; Perry, M.; Jolliffe, L.; Middleton, S.A.
Mol. Pharmacol., 2004, 66, 635.
81. Da Settimo, A.; Marini, A. M.; Primofiore, G.; Da Settimo, F.; Salerno, S.;
Viola, G.; Dalla Via, L.; Marciani Magno, S. Eur. J. Med. Chem. 1998, 33, 685.
82. Da Settimo, A.; Marini, A. M.; Primofiore, G.; Da Settimo, F.; Salerno, S.;
83. Dalla Via, L.; Gia, O.; Marciani Magno, S.; Da Settimo, A.; Primofiore, G.;
Da Settimo, F.; Simorini, F.; Marini, A. M. Eur. J. Med. Chem. 2002, 37, 475.
84. Dalla Via, L.; Marini, A. M.; Salerno, S.; Toninello, A. Biochem. Pharmacol.
2006, 72, 1657.
85. Marini, A. M.; Da Settimo, F.; Salerno, S.; La Motta, C.; Simorini, F.; Taliani, S.; Bertini, D.; Gia, O.; Dalla Via, L. J. Heterocycl. Chem. 2008, 45, 745.
86. Dalla Via, L.; Gia, O.; Marciani Magno, S.; Marini, A.M.; Salerno, S.; Da Settimo, F.; Fornaciari, G.; Simorini, F.; La Motta, C.; Taiani, S.; “Synthesis, Antiproliferative Activity And VEGFR-2 Inhibition of New Anilino-Substituted Thiopyrano Fused Pyrimidines”, XX National meeting on Medicinal Chemistry, September 12-16 2010 Abano Terme-Padova.
87. Da Settimo, A.; Marini, A.M.; Primofiore, G.; Da Settimo, F.; Salerno, S.; La Motta, C.; Pardi, G.; Ferrarini, P.L.; Mori, C.; J. Heterocyclic Chem, 2000, 37, 379-382.
88. Primofiore, G.; Marini, A.M.; Da Settimo, F.; Salerno, S.; Bertini, D.; Dalla Via, L.; Marciani Magno, S.; J. Heterocyclic Chem, 2003, 40, 783-788.
89. Bao, L.W.; Yong, H.L.; Jian, G.W.; Yi, M.; Zheng, M.L.; “Molecular design, synthesis and biological activities of amidines as new ketol-acid reductioisomerase inhibitors”, Elsevier, 2008, 19, 651-654.
90. Ekeley, John B.; Tieszen, Dirk V.; Ronzio, Anthony; “Some new amidine hydrochlorides”, Journal of the American Chemical Society, 1935, 5, 381.
91. C.E., Braun, “The Preparation of Some Structurally Related Monoguanidines”, J.Amer.Chem.Soc.,1933, 55, 1280-1284.
92. Yifeng, L.; Yajun, B.; Juan, Z.; Yangyang, L.; Junping, J.; Xiaoli, Q.;
“Optimization of the Conditions for Copper-Mediated N-Arylation of Heteroarylamines”, Eur. J. Org. Chem., 2007, 6084-6088.
93. Crowther, A.F.; Curd, F.H.S.; Richardson, D.N.; Rose, F.L.; J. Chem. Soc., 1948, 1636-1645.
94. Menichi, A.F.; Hubert-Habart, M.; Royer, R.; Eur. J. Med. Chem., 1974, 9, 11-13.
95. J.H., Short, U., Biermacher, D.A., Dunnigan, T.D., Leth, “Sympathetic Nervous System Blocking Agents. Derivatives of Guanidine and Related Compounds”, Journal of the American Chemical Society, 1963, 6, 275-283.
96. H., King, I.M., Tonkin, “Antiplasmodial Action and Chemical Constitution.
Part VIII. Guanidines and Diguanides”, J.Amer.Chem.Soc., 1946, 235, 1063- 1069.
