[1]
Ferlay, J.; Soerjomataram, I.; Dikshit, R.; Eser, S.; Mathers, C.; Rebelo, M.; Parkin, D.M.; Forman, D.; Bray, F. Cancer incidence and mortality worldwide: Sources, methods and major patterns in GLOBOCAN 2012. Int. J. Cancer, 2015, 136(5), E359-E386.
[2]
Normanno, N. Epidermal growth factor receptor (EGFR) signaling in cancer. Gene, 2006, 366(1), 2-16.
[3]
Barker, A.J.; Gibson, K.H.; Grundy, W.; Godfrey, A.A.; Barlow, J.J.; Healy, M.P.; Woodburn, J.R.; Ashton, S.E.; Curry, B.J.; Scarlett, L.; Henthorn, L.; Richards, L. Studies leading to the identification of ZD1839 (iressa™): An orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer. Bioorg. Med. Chem. Lett., 2001, 11(14), 1911-1914.
[4]
Moyer, J.D.; Barbacci, E.G.; Iwata, K.K.; Arnold, L.; Boman, B.; Cunningham, A.; DiOrio, C.; Doty, J.; Morin, M.J.; Moyer, M.P.; Neveu, M.; Pollack, V.A.; Pustilnik, L.R.; Reynolds, M.M.; Sloan, D.; Theleman, A.; Miller, P. Induction of apoptosis and cell cycle arrest by CP-358,774, an Inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res., 1997, 57(21), 4838.
[5]
Zhao, Q.; Shentu, J.; Xu, N.; Zhou, J.; Yang, G.; Yao, Y.; Tan, F.; Liu, D.; Wang, Y.; Zhou, J. Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors. Lung Cancer, 2011, 73(2), 195-202.
[6]
Chan, S.K.; Gullick, W.J.; Hill, M.E. Mutations of the epidermal growth factor receptor in non-small cell lung cancer - Search and destroy. Eur. J. Cancer, 2006, 42(1), 17-23.
[7]
Pao, W.; Katerina, A.P.; Gregory, J.R.; Romel, S.; Maureen, F.Z.; Mark, G.K. Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain. PLoS Med., 2005, 2(3), e73.
[8]
Yun, C.H.; Mengwasser, K.E.; Toms, A.V.; Woo, M.S.; Greulich, H.; Wong, K.K.; Meyerson, M.; Eck, M.J. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc. Natl. Acad. Sci. USA, 2008, 105(6), 2070-2075.
[9]
Ou, S.I. Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): A better mousetrap? A review of the clinical evidence. Crit. Rev. Oncol. Hematol., 2012, 83(3), 407-421.
[10]
aEngelman, J.A.; Zejnullahu, K.; Gale, C.M.; Lifshits, E.; Gonzales, A.J.; Shimamura, T.; Zhao, F.; Vincent, P.W.; Naumov, G.N.; Bradner, J.E.; Althaus, I.W.; Gandhi, L.; Shapiro, G.I.; Nelson, J.M.; Heymach, J.V.; Meyerson, M.; Wong, K.K.; Jänne, P.A. PF00299804, an Irreversible Pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res., 2007, 67(24), 11924.
bLi, D.; Ambrogio, L.; Shimamura, T.; Kubo, S.; Takahashi, M.; Chirieac, L.R.; Padera, R.F.; Shapiro, G.I.; Baum, A.; Himmelsbach, F.; Rettig, W.J.; Meyerson, M.; Solca, F.; Greulich, H.; Wong, K. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene, 2008, 27, 4702.
[11]
Cheng, H.; Nair, S.K.; Murray, B.W. Recent progress on third generation covalent EGFR inhibitors. Bioorg. Med. Chem. Lett., 2016, 26(8), 1861-1868.
[12]
Zhou, W.; Ercan, D.; Chen, L.; Yun, C.H.; Li, D.; Capelletti, M.; Cortot, A.B.; Chirieac, L.; Iacob, R.E.; Padera, R.; Engen, J.R.; Wong, K.K.; Eck, M.J.; Gray, N.S.; Jänne, P.A. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature, 2009, 462(7276), 1070-1074.
[13]
Walter, A.O.; Sjin, R.T.; Haringsma, H.J.; Ohashi, K.; Sun, J.; Lee, K.; Dubrovskiy, A.; Labenski, M.; Zhu, Z.; Wang, Z.; Sheets, M.; St-Martin, T.; Karp, R.; van Kalken, D.; Chaturvedi, P.; Niu, D.; Nacht, M.; Petter, R.C.; Westlin, W.; Lin, K.; Jaw-Tsai, S.; Raponi, M.; Van Dyke, T.; Etter, J.; Weaver, Z.; Pao, W.; Singh, J.; Simmons, A.D.; Harding, T.C.; Allen, A. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov., 2013, 3(12), 1404.
[14]
Finlay, M.R.V.; Anderton, M.; Ashton, S.; Ballard, P.; Bethel, P.A.; Box, M.R. Bradbury, R.H.; Brown, S.J.; Butterworth, S.; Campbell, A.; Chorley, C.; Colclough, N.; Cross, D.A.; Currie, G.S.; Gris,t M.; Hassall, L.; Hill, G.B.; James, D.; James, M.; Kemmitt, P.; Klinowska, T.; Lamont, G.; Lamont, S.G.; Martin, N.; McFarland, H.L.; Mellor, M.J.; Orme, J.P.; Perkins, D.; Perkins, P.; Richmond, G.; Smith, P.; Ward, R.A.; Waring, M.J.; Whittaker, D.; Wells, S.; Wrigley, G.L. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M re-sistance mutations that spares the wild type form of the receptor. J. Med. Chem., 2014, 57(20), 8249-8267.
[15]
Janne, P.A.; Yang, J.C.; Kim, D.W.; Planchard, D.; Ohe, Y.; Ra-malingam, S.S.; Ahn, M.J.; Kim, S.W.; Su, W.C.; Horn, L.; Haggstrom, D.; Felip, E.; Kim, J.H.; Frewer, P.; Cantarini, M.; Brown, K.H.; Dickinson, P.A.; Ghiorghiu, S.; Ranson, M. AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer. N. Engl. J. Med., 2015, 372(18), 1689-1699.
[16]
Wurz, R.P.; Pettus, H.L.; Ashton, K.; Brown, J.; Chen, J.J.; Herberich, B.; Hong, F-T.; Hu-Harrington, E.; Nguyen, T.; St. Jean, J.D., Jr Tadesse, Seifu.; Bauer, D.; Kubryk, M.; Zhan, J.; Cooke, K.; Mitchel, P.; Andrews, L. K.; Hsieh, F.; Hick-man, D.; Kalyanaraman, N.; Wu, T.; Reid, L.D.; Lobenhofer, E. K.; Andrews, D. A.; Everds, Nancy.; Guzman, R.; Parsons, A.T.; Hedley, J.S.; Tedrow, J.; Thiel, R.O.; Potter, M.; Ra-dinsky, R.; Beltran, J. P.; Tasker, A.S. Oxopyrido[2,3-d]pyrimidines as covalent L858R/T790M Mutant selective epidermal growth factor receptor (EGFR) inhibitors. ACS Med. Chem. Lett., 2015, 6(9), 987-992.
[17]
Xia, G.; Chen, W.; Zhang, J. Shaao, J.; Zhang, Y.; Huang, W.; Zhang, L.; Qi, W.; Sun, X.; Li, B.; Xiang, Z.; Ma, C.; Xu, J.; Deng, H.; Li, Y.; Li, P.; Mia, H.; Han, J.; Li, Y.; Shen, J.; Yu, Y. A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. J. Med. Chem., 2014, 57(23), 9889-9900.
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