ATP site-directed competitive and irreversible inhibitors of protein kinases

Medicinal Research Reviews

Volumn 20, Issue 1, 2000, Pages 28-57

  García Echeverría, Carlos ^a   Traxler, Peter ^a   Evans, Dean B ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Growth factors; Kinase inhibition; Pharmacophore model; Receptors; Structure based design

Indexed keywords

3 [(4,5 DIMETHYL 1H PYRROL 2 YL)METHYLENE] 1,3 DIHYDRO 2H INDOL 2 ONE; 4 (3 BROMOANILINO) 6,7 DIMETHOXYQUINAZOLINE; 6 (4 FLUOROPHENYL) 2,3 DIHYDRO 5 (4 PYRIDYL)IMIDAZO[2,1 B]THIAZOLE; ADENOSINE TRIPHOSPHATE; BALANOL; ERLOTINIB; FLAVOPIRIDOL; GEFITINIB; IMATINIB; OLOMOUCINE; PROTEIN KINASE INHIBITOR; ROSCOVITINE; RUBOXISTAURIN; STAUROSPORINE; UNCLASSIFIED DRUG;

DRUG ACTIVITY; DRUG BINDING; DRUG POTENCY; DRUG SOLUBILITY; DRUG SYNTHESIS; DRUG TARGETING; ENZYME INHIBITION; REVIEW; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; ANIMALS; ENZYME INHIBITORS; PROTEIN KINASE INHIBITORS; PROTEIN KINASES; SUBSTRATE SPECIFICITY;

EID: 0011672458     PISSN: 01986325     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1098-1128(200001)20:1<28::AID-MED2>3.0.CO;2-2     Document Type: Review

References (220)

1. Lawrence DS, Niu J. Pharmacol Thr 1998;77:81.
2. Profit AA, Lee TR, Lawrence DS. J Am Chem Soc 1999;121:280.
3. Strawn LM, Shawver LK. Expert Opin Invest Drug 1998;7:553.
4. Bridges AJ. Emerging Drug 1998;3:279.
5. Kelly AG, Laight A, Morris CO, Woodburn JR, Richmond GHP. In: 10th NCI-EORTC Symp New Drugs Cancer Ther Amsterdam; 1998.
6. Senderowicz AM, Headlee D, Stinson SF, Lush RM, Kalil N, Villalba L, Hill K, Steinberg SM, Figg WD, Tompkins A, Arbuck SG, Sausville EA. J Clin Oncol 1998;16:2986.
7. Mehta AB, Virchis AE, Jones DT, Hart SM, Wickremasinghe RG, Prentice HG, Yong KL, Csemak-Renner AMK, Ganeshaguru K. Blood 1997;90:3634.
8. Lavelle F. Expert Opin Invest Drug 1997;6:771.
9. Smith CM, Shindayalov IN, Veretnik S, Gribskov M, Taylor SS, Ten Eyck LF, Bourne PE. Trends Biochem Sci 1997;22:444.
10. Trumpp-Kallmeyer S, Rubin JR, Humblet C, Hamby JM, Showalter HDH. J Med Chem 1998;41:1752.
11. Trumpp-Kallmeyer S, Showalter HD. Chemtracts 1998;11:550.
12. Palmer BD, Trumpp-Kallmeyer S, Fry DW, Nelson JM, Showalter HDH, Denny WA. J Med Chem 1997;40:1519.
13. Furet P, Caravatti G, Lydon N, Priestle JP, Sowadski JM, Trinks U, Traxler P. J Comp-Aid Mol Des 1995;9:465.
14. Traxler P, Green J, Mett H, Séquin U, Furet P. J Med Chem 1999;42:1018.
15. Traxler P, Bold G, Frei J, Lang M, Lydon N, Mett H, Buchdunger E, Meyer T, Mueller M, Furet P. J Med Chem 1997;40:3601.
16. Traxler P, Furet P, Mett H, Buchdunger E, Meyer T, Lydon N. J Med Chem 1996;39:2285.
17. Adams JL, Lee D. Curr Opin Drug Disc Dev 1999;2:96.
18. McMahon G, Sun L, Liang C, Tang C. Cur Opin Drug Disc Dev 1998;1:131.
19. Traxler P. Expert Opin Ther Pat 1998;8:1599.
20. Traxler P. Expert Opin Ther Pat 1997;7:571.
21. Voldborg BR, Damstrup L, Spang-Thomsen M, Poulsen HS. Ann Oncol 1997;12:1197.
22. Heldin CH, & Ouml;stman A, Rönnstrand L. Biochim Biophys Acta 1998;1378:F79.
23. Neufeld G, Cohen T, Gengrinovitch S, Poltorak Z. FASEB J 1999; 13:9.
24. Klint P, Claesson-Welsh L. Front Biosci 1999;4:D165.
25. Garrington TP, Johnson GL. Curr Opin Cell Bio 1999;11:211.
26. Wang ZL, Canagarajah BJ, Boehm JC, Kassis S, Cobb MH, Young PR, Abdel-Meguid S, Adams JL, Goldsmith EJ. Structure 1998;6:1117.
27. Kyriakis JM, Avruch J. J Biol Chem 1996;271:24313.
28. Lee JC, Laydon JT, McDonnell PC, Gallagher TF, Kumar S, Green D, McNulty D, Blumenthal MJ, Heys JR, Landvatter SW, Strickler JE, et al. Nature 1994;372:739.
29. Pines J. Nature Cell Bio 1999;1:E73.
30. Fry DW, Kraker AJ, McMichael A, Ambroso LA, Nelson JM, Leopold WR, Connors RW, Bridges AJ. Science 1994;265:1093.
31. McMahon G, Shawver LK, Narog B, Tang PC, Hirth KP, inventors. Sugen WO-09810767; 1998.
32. Kunkel MW, Hook KE, Howard CT, Przybranowski S, Roberts BJ, Elliot WL, Leopold WR. Invest New Drug 1996;13:295.
33. Faust RA, Tawfic S, Davis AT, Ahmed K. Oral Oncol 1999;35:290.
34. Modjtahedi H, Affleck K, Stubberfield C, Dean C. Int J Oncol 1998;13:335.
35. Bos M, Mendelsohn J. Kim YM, Albanell J, Fry DW, Baselga J. Clin Cancer Res 1997;3:2099.
36. Jonström P, Fredriksson A, Thorell JO, Stone-Elander S. J Label Cpd Radiopharm 1998;XLI:623.
37. Gibson KH, inventor. Zeneca WO-09633980; 1996.
38. Woodburn JR, Barker AJ, Gibson KH, Ashton SE, Wakeling AE, Curry BJ, Scarlett L, Henthorn LR. Proc Am Assoc Cancer Res 1997;38:633.
39. Moyer JD, Barbacci EG, Iwata KK, Arnold L, Boman B, Cunningham A, DiOrio C, Doty J, Morin MJ, Moyer MP, Neveu M, Pollack VA, Pustilnik LR, Reynolds MM, Sloan D, Theleman A, Miller P. Cancer Res 1997;57:4838.
40. Iwata K, Miller PE, Barbacci EG, Arnold L, Doty J, DiOrio CI, Pustilnik LR, Reynolds M, Thelemann A, Sloan D, Moyer JD. Proc Am Assoc Cancer Res 1997;38:633.
41. Schnur RC, Arnold LD, inventors. Pfizer WO-09630347; 1996.
42. Myers MR, Spada AP, Maguire MP, Persons PE, inventors. Rhone-Poulenc Rorer Pharm US-05721237; 1998.
43. Barker AJ, Johnstone C, inventors. Zeneca WO-09730044; 1997.
44. Gibson KH, inventor. Zeneca WO-09738994; 1997.
45. Cockerill GS, Carter MC, McKeown SK, Vile S, Page MJ, Hudson AT, Barraciough P, Franzmann KW, inventors. Glaxo-Wellcome WO-09703069; 1997.
46. McKeown SK, Page MJ, Vile S. Walker AL, Hudson AT, Barraclough P, Franzmann KW, inventors. Glaxo-Wellcome WO-09713760; 1997.
47. Myers MR, Setzer NN, Spada AP, Persons PE, Ly CQ, Maguire MP, Zulli AL, Cheney DL, Zilberstein A, Johnson SE, Franks CF, Mitchell KJ. Bioorg Med Chem Lett 1997;7:421.
48. Myers MR, Setzer NN, Spada AP, Zulli AL, Hsu CYJ, Zilberstein A, Johnson SE, Hook KE, Jacoski MV. Bioorg Med Chem Lett 1997;7:417.
49. Gibson KH, Brundy W, Godfrey AA, Woodburn JR, Ashton SE, Curry BJ, Scarlett L, Barker AJ, Brown DS. Bioorg Med Chem Lett 1997;7:2723.
50. Bridges AJ, Zhou H, Cody DR, Rewcastle GF, McMichael A, Showalter HD, Fry DW, Kraker AJ, Denny WA. J Med Chem 1996;39:267.
51. Hsu CYJ, Johnson SE, Maguire MP, Myers MR, Persons PE, Spada AP, Zilberstein A, inventors. Rhone-Poulenc Rorer Pharm WO-09515758; 1995.
52. Rewcastle GF, Denny WA, Bridges AJ, Zhou H, Cody DR, McMichael A, Fry DW, J Med Chem 1995;38:3482.
53. Smaill JB, Palmer BD, Rewcastle GF, Denny WA, McNamara DJ, Dobrusin EM, Bridges AJ, Zhou H, Showalter HD, Winters RT, Leopold WR, Fry DW, Nelson JM, Slintak V, Elliot WL, Roberts BJ, Vincent PW, Patmore SJ. J Med Chem 1999;42:1803.
54. Fry DW, Bridges AJ, Denny WA, Doherty AM, Greis KD, Hicks JL, Hook KE, Keller PR, Leopold WR, Loo JA, McNamara DJ, Nelson JM, Sherwood V, Smaill JB, Trumpp-Kallmeyer S, Dobrusin EM. Proc Natl Acad Sci USA 1998;95:12022.
55. Bridges AJ, Denny WA, Dobrusin EM, Doherty AM, Fry DW, McNamara DJ, Showalter HD, Smaill JB, Zhou H, et al., inventors. Warner Lambert WO-09738983; 1997.
56. Vincent PW, Patmore SJ, Atkinson BE, Bridges AJ, Kirkish LS, Dudeck RC, Leopold WR, Zhou H, Elliott WL, Proc Am Assoc Cancer Res 1999;40:117.
57. Driscoll D, Steinkampf R, Patmore S, Elliot W, Klohs W. Proc Am Assoc Cancer Res 1999;40:121.
58. Bridges AJ, Denny WA, Dobrusin EM, Doherty AM, Fry DW, McNamara DJ, Showalter HD, Smaill JB, Zhou H, inventors. Warner Lambert WO-09738983; 1997.
59. Bridges AJ, inventor. Warner Lambert WO-09906396; 1999.
60. Bridges AJ, inventor. Warner Lambert WO-09906378; 1999.
61. Tang C, McMahon G, Weinberger H, Kutscher B, App H, inventors. Sugen WO-09850370; 1998.
62. Cockerill GS, Stubberfield C, Stables J, Carter M, Guntrip S, Smith K, Shaw R, Topley P. Proc Am Assoc Cancer Res 1999;40:117.
63. Hennequin LFA, Thomas AP, Johnstone C, Ple P, Stokes ESE, Ogilvie DJ, Dukes M, Wedge SR. Proc Am Assoc Cancer Res 1999;90:69.
64. Ogilvie DJ, Wedge SR, Dukes M, Kendrew J, Curwen JO, Thomas AP, Hennequin LFA, Ple P, Stokes ESE, Johnstone C, Wadsworth SA, Richmond GHP, Curry BJ. Proc Am Assoc Cancer Res 1999; 90:69.
65. Hennequin LFA, Ple P, Lohmann JJM, Thomas AP, inventors. Zeneca WO-09910349; 1999.
66. Thomas AP, Hennequin LFA, Ple P, inventors. Zeneca WO-09813350; 1998.
67. Thomas AP, Hennequin LFA, Johnstone C, Stokes ESE, Lohmann JJM, Clayton E, inventors. Zeneca WO-09813354; 1998.
68. App H, McMahon G, Tang PC, Gazit A, Levitzki A, inventors. Sugen US-5712395; 1998.
69. Lohmann JJM, Hennequin LFA, Thomas AP, inventors. Zeneca WO-09722596; 1997.
70. Thomas AP, Hennequin LFA, Johnstone C, inventors. Zeneca WO-09732856; 1997.
71. Thomas AP, Johnstone C, Hennequin LFA, inventors. Zeneca WO-09730035; 1997.
72. Thomas AP, Hennequin LFA, inventors. Zeneca WO-09734876; 1997.
73. Cobb JM, Fiorini MT, Goddard CR, Theoclitou ME, Abell C. Tetrahedron Lett 1999;40:1045.
74. Bridges AJ, Zhou H, Cody DR, Rewcastle GW, McMichael A, Showalter HD, Fry DW, Kraker AJ, Denny WA. J Med Chem 1996;39:267.
75. Zimmermann J, Buchdunger E, Mett H, Meyer T, Lydon NB. Bioorg Med Chem Lett 1997;7:187.
76. Druker BJ, Tamura S, Buchdunger E, Ohno S, Segal GM, Fanning S, Zimmermann J, Lydon NB. Nature Med 1996;2:561.
77. Buchdunger E, Zimmermann J, Mett H, Meyer T, Mueller M, Druker BJ, Lydon NB. Cancer Res 1996;56:100.
78. Zimmermann J, inventor. Ciba-Geigy WO-09509847; 1995.
79. Zimmermann J, inventor. Ciba-Geigy EP-0564409; 1993.
80. Zimmermann J, Buchdunger E, Mett H, Meyer T, Lydon NB, Traxler P. Bioorg Med Chem Lett 1996;6:1221.
81. Zimmermann J, Caravatti G, Mett H, Meyer T, Mueller M, Lydon NB, Fabbro D. Arch PharmWeinheim 1996;329:371.
82. Thomas AP, inventor. Zeneca WO-09515952; 1995.
83. Davis PD, Moffat DFC, Davis JM, Hutchings MC, inventor. Celltech Therapeutics WO-09719065; 1997.
84. Bridges AJ, Denny WA, Fry DW, Kraker AJ, Meyer RF, Rewcastle GF, Thompson AM, inventors. Warner Lambert WO-09519774; 1995.
85. Bridges AJ, Denny WA, Fry DW, Kraker AJ, Meyer RF, Rewcastle GF, Thompson AM, Showalter HD, inventors. Warner Lambert WO-09519970; 1995.
86. Thompson AM, Bridges AJ, Fry DW, Kraker AJ, Denny WA. J Med Chem 1995;38;3780.
87. Rewcastle GF, Palmer BD, Thompson AM, Bridges AJ, Cody DR, Zhou HM, Fry DW, McMichael A, Denny WA. J Med Chem 1996;39:1823.
88. Rewcastle GW, Murray DK, Elliott WL, Fry DW, Howard CT, Nelson JM, Roberts BJ, Vincent PW, Showalter HD, Winters RT, Denny WA. J Med Chem 1998;41:742.
89. Thompson AM, Murray DK, Elliott WL, Fry DW, Nelson JA, Showalter HD, Roberts BJ, Vincent PW, Denny WA. J Med Chem 1997;40:3915.
90. Cockerill GS, Carter MC, Guntrip SB, Smith KJ, inventors. Glaxo Group WO-09802438; 1998.
91. Cockerill GS, Carter MC, Guntrip SB, Smith KJ, inventors. Glaxo Group WO-09802437; 1998.
92. Cockerill GS, Guntrip SB, McKeown SK, Page MJ, Smith KJ, Vile S, Hudson AT, Barraclough P, Franzmann KW, et al., inventors. Glaxo Group WO-09713771; 1997.
93. Himmelsbach F, Dahmann G, von Ruden T, Metz T, inventors. Karl Thomae DE-19629652-A1; 1998.
94. Himmelsbach F, Dahmann G, von Ruden T, Metz T, inventors. Karl Thomae DE-1960831 -A1; 1997.
95. Blankley CJ, Boschelli DH, Doherty AM, Hamby JM, Klutchko SR, Panek RL, inventors. Warner Lambert WO-09634867; 1996.
96. Klutchko SR, Hamby JM, Boschelli DH, Wu Z, Kraker AJ, Amar A, Hartl BG, et al. J Med Chem 1998;41:3276.
97. Connolly CJC, Hamby JM, Schroeder MC, Barvian M, Lu GH, Panek RL, Amar A, Shen C, Kraker AJ, Fry DW, Klohs WD, Doherty AM. Bioorg Med Chem Lett 1997;7:2415.
98. Hamby JM, Connolly CJ, Schroeder MC, Winters RT, Showalter HD, Panek RL, Major TC, Olsewski B, Ryan MJ, Dahring T, Lu GH, Keiser J, Amar A, Shen C, Kraker AJ, Slintak V, Nelson JM, Fry DW, Bradford L, Hallak H, Doherty AM. J Med Chem 1997;40:2296.
99. Mohammadi M, Froum S, Hamby JM, Schroeder MC, Panek RL, Lu GH, Eliseenkova AV, Green D, Schlessinger J, Hubbard SR. EMBO J 1998;17:5896.
100. Kenyon BM, Voest EE, Chen CC, Flynn E, Folkman J, D'Amato RJ. Invest Ophthalmol Vis Sci 1996;37:1625.
101. Panek RL, Lu GH, Klutchko SR, Batley BL, Dahring TK, Hamby JM, Hallak H, Doherty AM, Keiser JA. J Pharmacol Exp Ther 1997;283:1433.
102. Boschelli DH, Wu Z, Klutchko SR, Showalter HD, Hamby JM, Lu GH, Major TC, Dahring T, Batley B, Panek RL, Keiser J, Hartl BG, Kraker AJ, Klohs WD, Roberts BJ, Patmore S, Elliott WL, Steinkampf R, Bradford L, Hallak H, Doherty AM. J Med Chem 1998;41:4365.
103. Rewcastle GF, Bridges AJ, Fry DW, Rubin JR, Denny WA. J Med Chem 1997;40:1820.
104. Himmelsbach F, Dahmann G, von Ruden T, Metz T, inventors. Karl Thomae WO-09732880; 1997.
105. Himmelsbach F, Dahmann G, von Ruden T, Metz T, inventors. Karl Thomae WO-09732882; 1997.
106. Traxler P, Furet P, Brill WD, inventors. Ciba-Geigy EP-00682027; 1995.
107. Traxler P, Bold G, Buchdunger E, Lang M, Mett H, Furet P. Book of abstracts. Dallas: 215th ACS Nat Meet; 1998.
108. Traxler P, Bold G, Lang M, Frei J, inventors. Novartis AG WO-09807726; 1998.
109. Traxler P, Frei J, Bold G, inventors. Novartis AG WO-09727199; 1997.
110. Traxler P, Bold G, Brill WD, Frei J, inventors. Novartis AG WO-09702266; 1997.
111. Missbach M, Jeschke M, Field JB, Muller M, Glatt M, Green J, Susa M. Bone 1999;24:437.
112. Missbach M, Green J, Susa M, Jeschke M, Buchdunger E, Mett H, Meyer T. Book of abstracts. Dallas: 215th ACS Nat Meet; 1998.
113. Altmann E, inventor. Novartis AG WO-09734895; 1997.
114. Altmann E, Missbach M, Widler L, inventors. Novartis AG WO-09732879; 1997.
115. Altmann E, Missbach M, Widler L, Maibaum JK, inventors. Novartis AG WO-09749706; 1997.
116. Altmann E, Widler L, Missbach M, inventors. Novartis AG WO-09728161;1997.
117. Missbach M, inventor. Ciba-Gcigy WO-09610028; 1996.
118. Henry JR, Rupert KC, Dodd JH, Turchi IJ, Wadsworth SA, Cavender DE, Fahmy B, Olini GC, Davis JE, Pellegrino-Gensey JL, Schafer PH, Siekeirka JJ. J Med Chem 1998;41:4196.
119. Hanke JH, Gardner JP, Dow RL, Changelian PS, Brisseite WH, Weringer EJ, Pollock BA, Connelly PA. J Biol Chem 1996;271:695.
120. Zhu X, Kim JL, Newcomb JR, Rose PE, Stover DR, Toledo LM, Zhao H, Morgenstern KA. Structure 1999;7:651.
121. Bold G, Frei J, Lang M, Traxler P, Furet P, inventors. Novartis AG WO-09814451; 1998.
122. Bold G, Frei J, Lang M, Traxler P, Furet P, inventors. Novartis AG WO-09814449; 1998.
123. Tang PC, Sun L, McMahon G, Shawver LK, Hirth KP, inventors. Sugen WO-09850356; 1998.
124. Tang C, Sun L, McMahon G, Hirth KP, Shawver LK, inventors. Sugen WO-09807695; 1998.
125. Sun L, Tran F, App H, Hirth P, McMahon G, Tang C. J Med Chem 1998;41:2588.
126. Fong TAT, Shawver LK, Sun L, Tang C, App H, Powell TJ, Kim YH, Schreck R, Wang X, Risau W, Ullrich A, Hirth KP, McMahon G. Cancer Res 1999;59:99.
127. Shawver LK, Strawn LM, Fong TAT, Antonian L, Sukbuntherng J, Powell TJ, Lipson K, Tang F, Tang C, Sun L, et al. Proc Am Assoc Cancer Res 1999;40:723.
128. Mohammadi M, McMahon G, Sun L, Tang C, Hirth P, Yeh BK, Hubbard SR, Schlessinger J. Science 1997;276:955.
129. Mohammadi M, Schlessinger J, Hubbard SR. Cell 1996;86:577.
130. Liang C, Sun L, Tran F, Schreck R, Tang C, Lipson KL, Shawver LK, McMahon G. Proc Am Assoc Cancer Res 1999;40:68.
131. Battistini C, Ermoli A, Vioglio S, Buzzetti F, Ballinari D, inventors. Pharmacia & Upjohn WO-09745409; 1997.
132. Battistini C, Vioglio S, Buzzetti F, Ballinari D, inventors. Pharmacia & Upjohn WO-09746551; 1997.
133. McNutt RW, Jung DK, Harris PA, Hunter RN, Veal JM, et al., inventors. Glaxo Group WO-09910325; 1999.
134. Lackey K, Chapman D, Crosby RM, Davenport E, Dickerson S, Gilmer TM, Griffin RJ, Hunter RN, Jung DK, Keith BR, Mahoney WB, McDonald OB, Mullin RJ, Rusnak DW, Wood E. Proc Am Assoc Cancer Res 1999;40:124.
135. Davis ST, Dickerson SH, Frye SV, Harris PA, Hunter RN, et al., inventors. Glaxo Group WO-09915500; 1999.
136. Luzzio MJ, Bramson N, Dickerson S, Frye SV, Harris P, Hassell AM, Holmes W, Hunter R, Kuyper L, Lackey K, Lovejoy B, Montana V, Roque W, Shewchuk L, Veal J, Walter D. Proc Am Assoc Cancer Res 1999;40:622.
137. Parker CW, Entsch B, Letham DS. Phytochem 1986;25:303.
138. Meijer L. Trends Cell Biol 1996;6:393.
139. Vesely J, Havlicek L, Strnad M, Blow JJ, Donella-Deana A, Pinna L, Letham DS, Kato J, Detivaud L. Eur J Biochem 1994;224:771.
140. Meijer L, Borgne A, Mulner O, Chong JPJ, Blow JJ, Inagaki N, Inagaki M, Delcros JG, Moulinoux JP. Eur J Biochem 1997;243:527.
141. Imbach P, Capraro HG, Furet P, Mett H, Meyer T, Zimmermann J. Bioorg Med Chem Lett 1999;9:91.
142. Legraverend M, Ludwig O, Bisagni E, Leclerc S, Meijer L. Bioorg Med Chem Lett 1998;8:793.
143. Havlicek L, Hanus J, Vesely J, Leclerc S, Meijer L, Shaw G, Strand M. J Med Chem 1997;40:408.
144. Zimmermann J, Capraro HG, Peterli P, Furet P, inventors. Novartis AG WO-09716452; 1997.
145. Gray NS, Wodicka L, Thunnissen AMWH, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, Leclerc S, Meijer L, Kim SH, Lockhart DJ, Schultz PG. Science 1998;281:533.
146. Norman TC, Gray NS, Koh JT, Schultz PG. J Am Chem Soc 1996; 118:7430.
147. Kim SH. Pure Appl Chem 1998;70:555.
148. De Azevedo WF, Leclerc S, Meijer L, Havlicek L, Strnad M, Kim SH. Eur J Biochem 1997;243:518.
149. Kim SH, Schulze-Gahmen U, Brandsen J, De Azevedo WF. Prog Cell Cycle Res 1996;2:137.
150. Schulze-Gahmen U, De Bondt HL, Kim SH. J Med Chem 1996;39:4540.
151. Russo AA, Jeffrey PD, Patten AK, Massagué J, Pavletich NP. Nature 1996;382:325.
152. Jeffrey PD, Russo AA, Polyak K, Gibbs E, Hurwitz J, Massagué J, Pavletich NP. Nature 1995;376: 313.
153. Schulze-Gahmen U, Brandsen J, Jones HD, Morgan DO, Meijer L, Vesely J, Kim SH. Protein Struc Func Gene 1995;22:378.
154. De Bondt HL, Rosenblatt J, Jancarlk J, Jones HD, Morgan DO, Kim SH. Nature 1993;363:595.
155. Chang YT, Gray NS, Rosania GR, Sutherlin DP, Kwon S, Norman TC, Sarohia R, Leost M, Meijer L, Schultz PG. Chem Bio 1999;6:361.
156. Fiorini MT, Abell C. Tetrahedron Lett 1998;39:1827.
157. Gray NS, Kwon S, Schultz PG. Tetrahedron Lett 1997;38:1161.
158. Schow SR, Mackman RL, Blum CL, Brooks E, Horsma AG, Joly A, Kerwar SS, Lee G, Shiftman D, Nelson MG, Wang X, Wick MM, Zhang X, Lum RT. Bioorg Med Chem Lett 1997;7:2697.
159. Nugiel DA, Cornelius LAM, Corbetl JW. J Org Chem 1997;62:201.
160. Lee JC, Badger AM, Griswold DE, Dunnington D, Truneh A, Votta B, White JR, Young PR, Bender PE. Ann NY Acad Sci 1993;696:149.
161. Tong L, Pav S, White DH, Rogers S, Crane KM, Cywin CL, Brown ML, Pargellis CA. Nature Struct Bio 1997;4:311.
162. Wilson KP, McCaff PG, Hsiao K, Pazhanisamy S, Galullo V, Bemis GW, Fitzgibbon MJ, Caron PR, Murcko HA, Su MSS. Chem Bio 1997;4:423.
163. Gallagher TF, Seibel GL, Kassis S, Laydon JT, Lee JC, Lee D, Boehm JC, Bender PE, Erhard KF, Krog AJ, Hofmann GA, Adams JL. Bioorg Med Chem Lett 1997;5:49.
164. Adams JL, Boehm JC, Kassis S, Gorycki PD, Webb EF, Hall R, Sorenson M, Lee JC, Ayrton A, Griswold DE, Gallagher TF. Bioorg Med Chem Lett 1998;8:3111.
165. Kumar S, McDonnell PC, Gum RJ, Hand AT, Lee JC, Young PR. Biochem Biophy Res Comm 1997;235:533.
166. Goedert M, Cuenda A, Craxton M, Jakes R, Cohen P. EMBO J 1997;16:3563.
167. Cohen P. Trends Cell Bio 1999:7:353.
168. Liverton NJ, Buthcer JW, Claremon DA, Bilodeau MT, inventors. Merck WO-09747618; 1997.
169. Jackson JR, Bolognese B, Hillegass L, Kassis S, Adams JL, Griswold DE, Winkler JD. J Pharmacol Exp Ther 1998;284:687.
170. Frantz B, Klatt T, Pang M, Parsons J, Rolando A, Williams H, Tocci MJ, O'Keefe SJ, O'Neill EA. Biochem 1998;37:13846.
171. Hanson GJ. Exp Opin Ther Patents 1997;7:729.
172. De Laszio SE, Visco D, Agarwal L, Chang L, Chin J, Croft G, Forsyth A, Fletcher D, Frantz B, Hacker C, et al. Bioorg Med Chem Lett 1998;8:2689.
173. De Laszio SE, Mantlo NB, Ponticello GS, Selnick HG, Liverton NJ, inventors. Merck WO-09705877; 1997.
174. De Laszlo SE, Mantlo NB, inventors. Merck WO-09716441; 1997.
175. De Laszlo SE, Mantlo NB, inventors. Merck WO-09716426; 1997.
176. De Laszlo SE, Mantlo NB, Ponticello GS, Selnick HG, Liverton NJ, inventors. Merck WO-09705878; 1997.
177. Hanson GJ, Liao S, inventors. Scarle WO-09852941; 1998.
178. Anantanarayan A, Clare M, Collins PW, Crich JZ, Devraj R, Flynn DL, Geng L, Hanson GJ, Koszyk FJ, Liao S, Partis R, Selness SR, South MS, Stealey MA, Weier RM, Xu X, inventors. Scarle WO-09852940; 1998.
179. Anantanarayan A, Clare M, Geng L, Hanson GJ, Partis R, Stealey MA, Weier RM, inventors. Searle WO-09852937; 1998.
180. Gallagher TF, Thompson SM, inventors. SmithKline Beecham WO-09733883; 1997.
181. Spohr UD, Malone MJ, Mantlo NB, inventors. Amgen WO-09824782; 1998.
182. Spohr UD, Malone MJ, Mantlo NB, Zablocki JA, inventors. Amgen WO-09824780; 1998.
183. Zablocki JA, Tartlton E, Rizzi JP, Mantlo NB, inventors. Amgen WO-09822457; 1998.
184. Liverton NJ, Butcher JW, Clairbone CF, Claremon DA, Libby BE, et al. J Med Chem 1999;42:2180.
185. Heimbrook DC, Huber HE, Stirdivant SM, Claremon D, Liverton NJ, Patrick DR, Selnick HG, et al. Proc Am Assoc Cancer Res 1998;39:558.
186. Kulanthaivel P, Hallock YF, Boros C, Hamilton SM, Janzen WP, Ballas LM, Loomis CR, Jiang JB. J Am Chem Soc 1993;115:6452.
187. Koide K, Bunnage ME, Paloma LG, Kanter JR, Taylor SS, Brunton LL, Nicolaou KC. Chem Bio 1995;2:601.
188. Defauw JM, Murphy MM, Jagdmann GE Jr, Hu H, Lampe JW, Hollinshead SP, Mitchell TJ, Crane HM, Heerding JM, Mendoza JS, Davis JE, Darges JW, Hubbard FR, Hall SE. J Med Chem 1996;39: 5215.
189. Lai YS, Mendoza JS, Jagdmann GE Jr, Menaldino DS, Biggers CK, Heerding JM, Wilson JW, Hall SE, Jiang JB, Janzen WP, Ballas LM. J Med Chem 1997;40:226.
190. Lai YS, Menaldino DS, Nichols JB, Jagdmann GE Jr, Mylott F, Gillespie J, Hall SE. Bioorg Med Chem Lett 1995;5:2151.
191. Mendoza JS, Jagdmann GE Jr, Gosnell PA. Bioorg Med Chem Lett 1995;5:2211.
192. Hu H, Hollinshead SP, Hall SE, Kalter K, Ballas LM. Bioorg Med Chem Lett 1996;6:973.
193. Crane HM, Menaldino DS, Jagdmann GE Jr, Darges JW, Buben JA. Bioorg Med Chem Lett 1995;5:2133.
194. Heerding JM, Lampe JW, Darges JW, Stamper ML. Bioorg Med Chem Lett 1995;5:1839.
195. Narayana N, Diller TC, Koide K, Bunnage ME, Nicolaou KC, Brunton LL, Xuong NH, Eyck LFT, Taylor SS. Biochem 1999;38:2367.
196. Sedlacek HH, Czech J, Naik R, Kaur G, Worland P, Losiewicz M, Parker B, Carlson B, Smith A, et al. Int J Oncol 1996;9:1143.
197. Patel V, Senderowicz AM, Adrian M, Pinto D Jr, Igishi T, Raffeld M, Quintanilla-Martinez L, Ensley JF, Sausville EA, Gulkind JS. J Clin Invest 1998;102:1674.
198. Drees M, Denny WA, Roth T, Labonte H, Mayo J, Malspeis L, Grever M, Sausville EA, Fiebig HH. Clin Cancer Res 1997;3:273.
199. Czech J, Hoffmann D, Naik R, Sedlacek HH. Int J Oncol 1995;6:31.
200. Losiewicz M, Carlson B, Kaur G, Sausville EA, Worland P. Biochem Biophy Res Comm 1994;201:589.
201. Kaur G, Stetler-Stevenson M, Sebers S, Worland P, Sedlacek HH, Myers C, Czech J, Naik R, Sausville EA. J Natl Cancer Inst 1992;84:1736.
202. De Azevedo WF, Mueller-Dieckmann HJ, Schulze-Gahmen U, Worland P, Sausville EA, Kim SH. Proc Natl Acad Sci USA 1996;93:2735.
203. Rueegg UT, Burgess GM. Trends Pharmacol Sci 1989;10:218.
204. Gescher A. Gen Pharmacol 1998;31:721.
205. Meyer T, Regenass U, Fabbro D, Alter E, Rösel J, Müller M, Caravatti G, Matter A. Int J Cancer 1989;43:851.
206. Utz I, Hofer S, Regenass U, Hilbe W, Thaler J, Grunicke H, Hofmann J. Int J Cancer 1994;57:104.
207. Takahashi I, Saitoh Y, Yoshida M, Sano H, Nakano H, Morimoto M, Tamaoki T. J Antibiot 1989;42:571.
208. Takahashi I, Kobayashi E, Asano K, Yoshida M, Nakano H. J Antibiot 1987;40:1782.
209. Nomoto H, Nakano H, Takahashi I, Tamaoki T, Tomita F, Kawamoto I, Asano K, Morimoto M, inventors. Kyowa Hakko Kogyo EP-0238011; 1987.
210. Camoratto AM, Jani JP, Angeles T, Maroney AC, Sanders CY, Murakata C, Neff NT, Vaught JL, Isaacs JT, Dionne CA. Int J Cancer 1997;72:673.
211. Dionne CA, Camoratto AM, Jani JP, Emerson E, Neff NT, Vaught JL, Murakata C, Djakiew D, Lamb J, Bova S, George D, Isaacs JT. Clin Cancer Res 1998;4:1887.
212. Hudkins RL, Iqbal M, Park CH, Goldstein J, Herman J, Shek E, Murakata C, Mallamo JP, Bioorg Med Chem Lett 1998;8:1873.
213. Spacey GD, Uings IJ, Slater M, Hirst S, Bonser RW. Biochem Pharmacol 1998;55:261.
214. Jirousek MR, Gillig JR, Gonzalez CM, Heath WF, McDonald JH III, Neel DA, Rito CJ, Singh U, Stramm LE. J Med Chem 1996;39:2664.
215. Ishii H, Jirousek MR, Koya D, Takagi C, Xia P, Clemont A, Bursell SE, Kern TS, Ballas LM, Heath WF, Stramm LE, Feener EP, King GL. Science 1996;272:728.
216. Inoguchi T, Battan R, Handler E, Sportsman JR, Health W, King GL. Proc Natl Acad Sci USA 1992;89:11059.
217. Riley DA, Simpkins NS, Moffat D. Tetrahedron Lett 1999;40:3929.
218. Bold G, Frei J, Traxler P, Altmann KH, Mett H, Stover DR, Wood J, inventors. Novartis AG WO9835958; 1998.
219. Wood J, Buchdunger E, Cozens R, Hoffman F, Mestan J, Mett H, Mueller M, Roesel J, Schnell C, Stover DR, Wood-Cook K, Bold G, Frei J, et al. Proc Am Assoc Cancer Res 1998;39:96.
220. Bishop AC, Kung CY, Shah K, Witucki L, Shokat KM, Liu Y. J Am Chem Soc 1999;121:627.