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Pyridone-based c-Met inhibitors selective over a number of kinases have been described
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Pyridone-based c-Met inhibitors selective over a number of kinases have been described: Schroeder, G. M.; An, Y.; Cai, Z.-W.; Chen, X.-T.; Clark, C.; Cornelius, L. A. M.; Dai, J.; Gullo-Brown, J.; Gupta, A.; Henley, B.; Hunt, J. T.; Jeyaseelan, R.; Kamath, A.; Kim, K.; Lippy, J.; Lombardo, L. J.; Manne, V.; Oppenheimer, S.; Sack, J. S.; Schmidt, R. J.; Shen, G.; Stefanski, K.; Tokarski, J. S.; Trainor, G. L.; Wautlet, B. S.; Wei, D.; Williams, D. K.; Zhang, Y.; Zhang, Y.; Fargnoli, J.; Borzilleri, R. M. Discovery of N -(4-(2-Amino-3- chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1, 2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily J. Med. Chem. 2009, 52, 1251-1254
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As we have postulated previously, it might be useful to employ two types of c-Met inhibitors to treat c-Met-dependent tumors: very potent and selective class I inhibitors of wild-type c-Met and class II inhibitors that inhibit a wider range of c-Met mutations than those inhibited by class I molecules, thereby offering more treatment options for cancer patients. ()
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As we have postulated previously, it might be useful to employ two types of c-Met inhibitors to treat c-Met-dependent tumors: very potent and selective class I inhibitors of wild-type c-Met and class II inhibitors that inhibit a wider range of c-Met mutations than those inhibited by class I molecules, thereby offering more treatment options for cancer patients. Dussault, I.; Bellon, S. F. c-Met inhibitors with different binding modes Cell Cycle 2008, 7 (9) 1157-1160
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DOI 10.1021/jm201331s.
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Liu, L.; Norman, M. H.; Lee, M.; Xi, N.; Siegmund, A.; Boezio, A.; Booker, S.; Choquette, D.; D'Angelo, N. D.; Germain, J.; Yang, Y.; Zhang, Y.; Bellon, S. F.; Whittington, D. A.; Harmange, J.-C.; Dominguez, C.; Kim, T.-S.; Dussault, I. Structure-Based Design of Novel Class II c-Met Inhibitors: 2. SAR and Kinase Selectivity Profiles of the Pyrazolone Series. J. Med. Chem. 2012, DOI 10.1021/jm201331s.
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(2012)
J. Med. Chem.
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Liu, L.1
Norman, M.H.2
Lee, M.3
Xi, N.4
Siegmund, A.5
Boezio, A.6
Booker, S.7
Choquette, D.8
D'Angelo, N.D.9
Germain, J.10
Yang, Y.11
Zhang, Y.12
Bellon, S.F.13
Whittington, D.A.14
Harmange, J.-C.15
Dominguez, C.16
Kim, T.-S.17
Dussault, I.18
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