1. G. Vlahovic, J. Crawford, “Activation of Tyrosine Kinases in Cancer”, The Oncologist (2003), 8: 531-538.

(1)

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), 3

^th

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.

(2)

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. J. Baselga, “Epidermal growth factor receptor pathway inhibitors”, Update on Cancer Therapeutics (2006) I: 299-310.

15. R.S. Herbst, “Targeting the epidermal growth factor receptor in cancer therapy”, Expert Opinion on Investigational Drugs (2002), 11: 837-849.

16. M.L. Janmaat, G. Giaccone, “Small-Molecule Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors”, The Oncologist (2003), 8: 576-586.

17. R.L. Comis, “The Current Situation: Erlotinib (Tarceva

^®

) and Gefitinib (Iressa

^®

) in Non-Small Cell Lung Cancer”, The Oncologist (2005), 10: 467-470.

18. 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.

(3)

19. S. Klein, A. Levitzki, “Targeting the EGFR and the PKB pathway in cancer”, Current Opinion in Cell Biology (2009), 21: 185–193.

20. 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.

21. M.A. Gieseg, C. De Bock, L.R. Ferguson, W.A. Denny, “Evidence for epidermal growth factor receptor-enhanced chemosensitivity in combination of cisplatin and new irreversible tyrosine kinase inhibitor CI-1033”, Anticancer Drugs (2001), 8: 683-90.

22. 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

23. N. Ferrara, “Role of vascular endothelial growth factor in regulation of physiological angiogenesis”, Am. J. Physiol. Cell Physiol. (2001), 280: 1358- 1366.

24. A. Morabito, E. De Maio, M. Di Maio, N. Normanno, F. Perrone, “Tyrosine Kinase Inhibitors of Vascular Endothelial Growth Factor Receptors in Clinical Trials: Current Status and Future Directions”, The Oncologist (2006), 11: 753- 764.

25. N. Rahimi, “Vascular endothelial growth factor receptors: Molecular mechanism of activation and therapeutic potentials”, Experimental Eye Research (2006), 83:

1005-1016.

(4)

26. T. Veikkola, M. Karkkainen, L. Claesson-Welsh, and K. Alitalo, “Regulation of Angiogenesis via Vascular Endothelial Growth Factor Receptors”, Cancer Research (2000), 60: 203-212.

27. 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.

28. J. Tabernero, “The Role of VEGF and EGFR Inhibition: Implications for Combining Anti-VEGF and Anti-EGFR Agents”, Molecular Cancer Research (2007), 5: 203-220.

29. 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

30. 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.

31. 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.

32. 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.

33. A. Vulpetti, R. Bosotti, Sequence and structural analysis of kinase ATP pocket

residues, Il Farmaco, (2004), 59: 759-765.

(5)

34. 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, 41, 1752-1763 (1998).

35. 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, 40, 1519-1529 (1997).

36. 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.

37. 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.

38. 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.

39. 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 (Iressa

^TM

): 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.

40. G. Bold et al. “New Anilino Phthalazines as Potent and Orally Well Absorbed

(6)

Tumor-Driven angiogenesis” Journal of Medicinal Chemistry (2000), 43: 2310- 2323

41. G. W. Rewcastle, B.D. Palmer, A.M. Thompson, A.J. Bridges, D.R. Cody, H.

Zhou, D.W. Fry, A. McMichael, W.A. Denny, “Tyrosine Kinase Inhibitors. 10.

Isomeric 4-[(3-Bromophenyl)amino]pyrido[d]-pyrimidines Are Potent ATP Binding Site Inhibitors of the Tyrosine Kinase Function of the Epidermal Growth Factor Receptor”, Journal of Medicinal Chemistry (1996), 36: 1823- 1835

42. P. Traxler, F. Pascal, H. Mett, E. Buchdunger, T. Meyer, N. Lydon, “4- (Phenylamino)pyrrolopyrimidines: Potent and Selective, ATP Site Directed Inhibitors of the EGF-Receptor Protein Tyrosine Kinase”, Journal of Medicinal Chemistry (1996) 39 : 2285-2292.

43. P. Traxler, G. Bold, J. Frei, M. Lang, N. Lydon, H. Mett, E. Buchdunger, T.

Meyer, M. Mueller, P. Furet, “Use of pharmacophore model for the design of EGFR tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines”, Journal of Medicinal Chemistry (1997), 40: 3601-3616.

44. S. Schenone, O. Bruno, A. Ranise, F. Bondavalli, C. Brullo, P. Fossa, L. Mosti, G. Menozzi, F. Carraro, A. Naldini, C. Bernini, F. Manetti, M. Botta, “New pirazolo[3,4-d]pyrimidines endowed with A431 antiproliferative activity and inhibitory properties of Src phosphorylation”, Biorganic & Medicinal Chemistry Letters (2004), 14: 2511-2517.

45. C.N. Cavasotto, M.A. Ortiz, R.A. Abagyan, F.J. Piedrafita, “In silico

identification of novel EGFR inhibitors with antiproliferative activity against

cancer cells”, Biorganic & Medicinal Chemistry Letters (2006), 16: 1969-1974.

(7)

46. S. Moro, P. Braiuca, F. Deflorian, C. Ferrari, G. Pastorin, P. Cacciari, P.G.

Baraldi, K. Varani, P.A. Borea, G. Spalluto “ Combined Target-Based and Ligand-Based Drug Design Approach as Tool To Define a Novel 3D- Pharmacophore Model of Human A

3

Adenosine receptor Antagonists:

Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine Derivatives as a Key Study”

Journal of Medicinal Chemistry (2005), 48: 152-162.

47. F.A. Harden, R.J. Quinn, P.J. Scammells, “Synthesis and Adenosine Receptor Affinity of a Series of Pyrazolo[3,4-d]pyrimidine Analogues of 1- Methylisoguanosine”, Journal of Medicinal Chemistry (1991), 34: 2892-2898.

48. G. Ege, H. Franz, Aminopyrazoles. IV (1). “Pyrazol-3- and 5-amine form 2,3-

Dihaloalkanenitriles or 3-Chloroacrylonitirles and Hydrazines”, Journal of

Heterocyclic Chemistry (1982), 19: 1267-1273