1. University of Nottingham, UK

Abstract

Contents

GtoPdb is an expert-driven guide to pharmacological targets and the substances that act on them. GtoPdb is a reference work which is most usefully represented as an on-line database. As in any publication this work should be appropriately cited, and the papers it cites should also be recognized. This document provides a citation for the relevant parts of the database, and also provides a reference list for the research cited by those parts. For further details see [15].

Please note that the database version for the citations given in GtoPdb are to the most recent preceding version in which the family or its subfamilies and targets were substantially changed. The links below are to the current version. If you need to consult the cited version, rather than the most recent version, please contact the GtoPdb curators.

Database links

References

1. Abdelmalek CM, Hu Z, Kronenberger T, Küblbeck J, Kinnen FJM, Hesse SS, Malik A, Kudolo M, Niess R and Gehringer M et al.. (2022) Gefitinib-Tamoxifen Hybrid Ligands as Potent Agents against Triple-Negative Breast Cancer. J Med Chem 65: 4616-4632 [PMID:35286086]
2. Aertgeerts K, Skene R, Yano J, Sang BC, Zou H, Snell G, Jennings A, Iwamoto K, Habuka N and Hirokawa A et al.. (2011) Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein. J Biol Chem 286: 18756-65 [PMID:21454582]
3. Amishima M, Munakata M, Nasuhara Y, Sato A, Takahashi T, Homma Y and Kawakami Y. (1998) Expression of epidermal growth factor and epidermal growth factor receptor immunoreactivity in the asthmatic human airway. Am J Respir Crit Care Med 157: 1907-12 [PMID:9620926]
4. Anastassiadis T, Deacon SW, Devarajan K, Ma H and Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol 29: 1039-45 [PMID:22037377]
5. Antczak C, Mahida JP, Bhinder B, Calder PA and Djaballah H. (2012) A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen 17: 885-99 [PMID:22573732]
6. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM and Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol 4: 691-9 [PMID:18849971]
7. Arnett SO, Teillaud JL, Wurch T, Reichert JM, Dunlop C and Huber M. (2011) IBC's 21st Annual Antibody Engineering and 8th Annual Antibody Therapeutics International Conferences and 2010 Annual Meeting of the Antibody Society. December 5-9, 2010, San Diego, CA USA. MAbs 3: 133-52 [PMID:21304271]
8. AstraZeneca. AZD9291. http://openinnovation.astrazeneca.com/what-we-offer/compound/azd9291/. Accessed on 12/09/2014.
9. Badura L, Swanson T, Adamowicz W, Adams J, Cianfrogna J, Fisher K, Holland J, Kleiman R, Nelson F and Reynolds L et al.. (2007) An inhibitor of casein kinase I epsilon induces phase delays in circadian rhythms under free-running and entrained conditions. J Pharmacol Exp Ther 322: 730-8 [PMID:17502429]
10. Barf T and Kaptein A. (2012) Irreversible protein kinase inhibitors: balancing the benefits and risks. J Med Chem 55: 6243-62 [PMID:22621397]
11. Barlaam B, Anderton J, Ballard P, Bradbury RH, Hennequin LF, Hickinson DM, Kettle JG, Kirk G, Klinowska T and Lambert-van der Brempt C et al.. (2013) Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors. ACS Med Chem Lett 4: 742-6 [PMID:24900741]
12. Bhattacharjee D, Bakar J, Chitnis SP, Sausville EL, Ashtekar KD, Mendelson BE, Long K, Smith JC, Heppner DE and Sheltzer JM. (2023) Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor. Cell Chem Biol 30: 1211-1222.e5 [PMID:37827156]
13. Bradshaw JM, McFarland JM, Paavilainen VO, Bisconte A, Tam D, Phan VT, Romanov S, Finkle D, Shu J and Patel V et al.. (2015) Prolonged and tunable residence time using reversible covalent kinase inhibitors. Nat Chem Biol 11: 525-31 [PMID:26006010]
14. Bridges AJ, Zhou H, Cody DR, Rewcastle GW, McMichael A, Showalter HD, Fry DW, Kraker AJ and Denny WA. (1996) Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem 39: 267-76 [PMID:8568816]
15. Buneman P, Christie G, Davies JA, Dimitrellou R, Harding SD, Pawson AJ, Sharman JL and Wu Y. (2020) Why data citation isn't working, and what to do about it Database 2020 [PMID:32367113]
16. Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, Chaves J, Wierda WG, Awan FT and Brown JR et al.. (2016) Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. N Engl J Med 374: 323-32 [PMID:26641137]
17. Cai X, Zhai HX, Wang J, Forrester J, Qu H, Yin L, Lai CJ, Bao R and Qian C. (2010) Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. J Med Chem 53: 2000-9 [PMID:20143778]
18. Campbell JE, Dineen TA, Broojmans N, Brubaker JD, Eno MS, Kim JL, Ozen A, Perola E, Williams BD and Wilson D et al.. (2021) Inhibitors of mutant forms of EGFR Patent number: WO2021133809A1. Assignee: Blueprint Medicines Corporation. Priority date: 23/12/2019. Publication date: 07/01/2021.
19. Campbell P, Morton PE, Takeichi T, Salam A, Roberts N, Proudfoot LE, Mellerio JE, Aminu K, Wellington C and Patil SN et al.. (2014) Epithelial inflammation resulting from an inherited loss-of-function mutation in EGFR. J Invest Dermatol 134: 2570-2578 [PMID:24691054]
20. Carlomagno F, Vitagliano D, Guida T, Ciardiello F, Tortora G, Vecchio G, Ryan AJ, Fontanini G, Fusco A and Santoro M. (2002) ZD6474, an orally available inhibitor of KDR tyrosine kinase activity, efficiently blocks oncogenic RET kinases. Cancer Res 62: 7284-90 [PMID:12499271]
21. Cha MY, Ha TH, Jeon JY, Jo MG, Kang SJ, Kim MS, Kim MR, Kwak EJ, Lee JY, Lee KO and Suh KH. (2012) Novel fused pyrimidine derivatives for inhibition of tyrosine kinase activity Patent number: WO2011162515. Assignee: Hanmi Holdings Co. , Ltd.. Priority date: 30/06/2010. Publication date: 03/05/2012.
22. Chang CJ and Geahlen RL. (1992) Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents. J Nat Prod 55: 1529-60 [PMID:1479375]
23. Chang GP, Cheung AF, Haney W, Lunds BM and Prinz B. (2018) A protein binding nkg2d, cd16 and a tumor-associated antigen. Patent number: WO2018217947A1. Assignee: Dragonfly Therapeutics, Inc.. Priority date: 23/05/2017. Publication date: 29/11/2018.
24. Changelian PS, Moshinsky D, Kuhn CF, Flanagan ME, Munchhof MJ, Harris TM, Whipple DA, Doty JL, Sun J and Kent CR et al.. (2008) The specificity of JAK3 kinase inhibitors. Blood 111: 2155-7 [PMID:18094329]
25. Chen H, Lai M, Zhang T, Chen Y, Tong L, Zhu S, Zhou Y, Ren X, Ding J and Xie H et al.. (2022) Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations. J Med Chem 65: 6840-6858 [PMID:35446588]
26. Cheng H, Nair SK and Murray BW. (2016) Recent progress on third generation covalent EGFR inhibitors. Bioorg Med Chem Lett 26: 1861-8 [PMID:26968253]
27. Cheng M, Yu X, Lu K, Xie L, Wang L, Meng F, Han X, Chen X, Liu J and Xiong Y et al.. (2020) Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders. J Med Chem 63: 1216-1232 [PMID:31895569]
28. Cho HS and Leahy DJ. (2002) Structure of the extracellular region of HER3 reveals an interdomain tether. Science 297: 1330-3 [PMID:12154198]
29. Cho HS, Mason K, Ramyar KX, Stanley AM, Gabelli SB, Denney DW and Leahy DJ. (2003) Structure of the extracellular region of HER2 alone and in complex with the Herceptin Fab. Nature 421: 756-60 [PMID:12610629]
30. Cockerill S, Stubberfield C, Stables J, Carter M, Guntrip S, Smith K, McKeown S, Shaw R, Topley P and Thomsen L et al.. (2001) Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. Bioorg Med Chem Lett 11: 1401-5 [PMID:11378364]
31. Comez D, Glenn J, Anbuhl SM, Heukers R, Smit MJ, Hill SJ and Kilpatrick LE. (2022) Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living cells. Front Immunol 13: 1006718 [PMID:36505413]
32. Coumar MS, Chu CY, Lin CW, Shiao HY, Ho YL, Reddy R, Lin WH, Chen CH, Peng YH and Leou JS et al.. (2010) Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification. J Med Chem 53: 4980-8 [PMID:20550212]
33. Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA and Mellor MJ et al.. (2014) AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov 4: 1046-61 [PMID:24893891]
34. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK and Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol 29: 1046-51 [PMID:22037378]
35. Engelhardt H, Böse D, Petronczki M, Scharn D, Bader G, Baum A, Bergner A, Chong E, Döbel S and Egger G et al.. (2019) Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. J Med Chem 62: 10272-10293 [PMID:31689114]
36. Enomoto Y, Orihara K, Takamasu T, Matsuda A, Gon Y, Saito H, Ra C and Okayama Y. (2009) Tissue remodeling induced by hypersecreted epidermal growth factor and amphiregulin in the airway after an acute asthma attack. J Allergy Clin Immunol 124: 913-20.e1-7 [PMID:19895983]
37. Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M and Knapp S. (2007) A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci USA 104: 20523-8 [PMID:18077363]
38. Fitzgerald JB, Johnson BW, Baum J, Adams S, Iadevaia S, Tang J, Rimkunas V, Xu L, Kohli N and Rennard R et al.. (2014) MM-141, an IGF-IR- and ErbB3-directed bispecific antibody, overcomes network adaptations that limit activity of IGF-IR inhibitors. Mol Cancer Ther 13: 410-25 [PMID:24282274]
39. Flohr A, Mayweg A, Trainor G, Epstein DM, O'Connor M, Buck E and Arista L. (2021) Tyrosine kinase inhibitor compositions, methods of making and methods of use Patent number: US11034672B1. Assignee: Black Diamond Therapeutics Inc. Priority date: 25/09/2018. Publication date: 15/06/2021.
40. Foon KA, Yang XD, Weiner LM, Belldegrun AS, Figlin RA, Crawford J, Rowinsky EK, Dutcher JP, Vogelzang NJ and Gollub J et al.. (2004) Preclinical and clinical evaluations of ABX-EGF, a fully human anti-epidermal growth factor receptor antibody. Int J Radiat Oncol Biol Phys 58: 984-90 [PMID:14967460]
41. Fry DW, Bridges AJ, Denny WA, Doherty A, Greis KD, Hicks JL, Hook KE, Keller PR, Leopold WR and Loo JA et al.. (1998) Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci USA 95: 12022-7 [PMID:9751783]
42. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R and Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J 451: 313-28 [PMID:23398362]
43. Garner AP, Sprague EAR, Ettenberg SA, Kunz C, Haubst N and Elis W.. (2014) Antibodies for epidermal growth factor receptor 3 (HER3). Patent number: US8735551 B2. Assignee: Novartis Ag.. Priority date: 20/08/2010. Publication date: 27/05/2014.
44. Gaul MD, Guo Y, Affleck K, Cockerill GS, Gilmer TM, Griffin RJ, Guntrip S, Keith BR, Knight WB and Mullin RJ et al.. (2003) Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines. Bioorg Med Chem Lett 13: 637-40 [PMID:12639547]
45. Gavai AV, Fink BE, Fairfax DJ, Martin GS, Rossiter LM, Holst CL, Kim SH, Leavitt KJ, Mastalerz H and Han WC et al.. (2009) Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases. J Med Chem 52: 6527-30 [PMID:19821562]
46. Gazit A, Osherov N, Posner I, Yaish P, Poradosu E, Gilon C and Levitzki A. (1991) Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem 34: 1896-907 [PMID:1676428]
47. Gazit A, Yaish P, Gilon C and Levitzki A. (1989) Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem 32: 2344-52 [PMID:2552117]
48. Gendreau SB, Ventura R, Keast P, Laird AD, Yakes FM, Zhang W, Bentzien F, Cancilla B, Lutman J and Chu F et al.. (2007) Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647. Clin Cancer Res 13: 3713-23 [PMID:17575237]
49. Geuijen CAW, De Nardis C, Maussang D, Rovers E, Gallenne T, Hendriks LJA, Visser T, Nijhuis R, Logtenberg T and de Kruif J et al.. (2018) Unbiased Combinatorial Screening Identifies a Bispecific IgG1 that Potently Inhibits HER3 Signaling via HER2-Guided Ligand Blockade. Cancer Cell 33: 922-936.e10 [PMID:29763625]
50. Goldstein NI, Giorgio NA, Jones ST and Saldanha JW. (2006) Epidermal growth factor; nucleic acids, protein which binds to epidermal growth factor receptors; genetic engineering. Patent number: US7060808. Assignee: Imclone Systems Incorporated. Priority date: 07/06/1995. Publication date: 13/06/2006.
51. Grassot J, Mouchiroud G and Perrière G. (2003) RTKdb: database of Receptor Tyrosine Kinase. Nucleic Acids Res 31: 353-8 [PMID:12520021]
52. Graus-Porta D, Beerli RR, Daly JM and Hynes NE. (1997) ErbB-2, the preferred heterodimerization partner of all ErbB receptors, is a mediator of lateral signaling. EMBO J 16: 1647-55 [PMID:9130710]
53. Gundla R, Kazemi R, Sanam R, Muttineni R, Sarma JA, Dayam R and Neamati N. (2008) Discovery of novel small-molecule inhibitors of human epidermal growth factor receptor-2: combined ligand and target-based approach. J Med Chem 51: 3367-77 [PMID:18500794]
54. Han L, Zhang X, Wang Z, Zhang X, Zhao L, Fu W, Liang X, Zhang Z and Wang Y. (2021) SH-1028, An Irreversible Third-Generation EGFR TKI, Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer. Front Pharmacol 12: 665253 [PMID:33986687]
55. Hanke JH, Gardner JP, Dow RL, Changelian PS, Brissette WH, Weringer EJ, Pollok BA and Connelly PA. (1996) Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J Biol Chem 271: 695-701 [PMID:8557675]
56. Harms BD, Kearns JD, Su SV, Kohli N, Nielsen UB and Schoeberl B. (2012) Optimizing properties of antireceptor antibodies using kinetic computational models and experiments. Meth Enzymol 502: 67-87 [PMID:22208982]
57. Hasako S, Terasaka M, Abe N, Uno T, Ohsawa H, Hashimoto A, Fujita R, Tanaka K, Okayama T and Wadhwa R et al.. (2018) TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther 17: 1648-1658 [PMID:29748209]
58. Holgate ST. (2000) Epithelial damage and response. Clin Exp Allergy 30 Suppl 1: 37-41 [PMID:10849473]
59. Hu S, Xie G, Zhang DX, Davis C, Long W, Hu Y, Wang F, Kang X, Tan F and Ding L et al.. (2012) Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors. Bioorg Med Chem Lett 22: 6301-5 [PMID:22959248]
60. Huang W-S, Gong Y, Li F, Bencivenga NE, Dalgarno DC, Kohlmann A, Shakespeare WC, Thomas RM, Zhu X and West AV et al.. (2015) Heteroaryl compounds for kinase inhibition Patent number: WO2015195228A1. Assignee: Ariad Pharmaceuticals, Inc.. Priority date: 19/06/2014. Publication date: 23/12/2015.
61. Huang Z and Dong Y. (2012) Quinazoline derivatives substituted by aniline, preparation method and use thereof Patent number: WO2012027960A1. Assignee: Shandong Xuanzhu Pharma Co Ltd. Priority date: 30/08/2011. Publication date: 30/03/2012.
62. Jarantow SW, Bushey BS, Pardinas JR, Boakye K, Lacy ER, Sanders R, Sepulveda MA, Moores SL and Chiu ML. (2015) Impact of Cell-surface Antigen Expression on Target Engagement and Function of an Epidermal Growth Factor Receptor × c-MET Bispecific Antibody. J Biol Chem 290: 24689-704 [PMID:26260789]
63. Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez J, Xu C, Rhee K, Chen T and Zhang H et al.. (2016) Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature 534: 129-32 [PMID:27251290]
64. Jiang J, Li S, Shan X, Wang L, Ma J, Huang M, Dong L and Chen F. (2020) Preclinical safety profile of disitamab vedotin：a novel anti-HER2 antibody conjugated with MMAE. Toxicol Lett 324: 30-37 [PMID:31877330]
65. Jiang Y. (2015) Pyrimidine or pyridine compound, and preparation method and pharmaceutical application thereof Patent number: CN105085489A. Assignee: Yifang Biotechnology (Shanghai) Co.,Ltd.; Betta Pharmaceuticals Co Ltd. Priority date: 01/04/2015. Publication date: 25/11/2015.
66. Johnson LS, Huang L, Tuaillon N and Bonvini E.. (2014) HER2/neu-specific antibodies and methods of using same. Patent number: US8802093 B2. Assignee: Macrogenics, Inc.. Priority date: 02/04/2008. Publication date: 12/08/2014.
67. Jones JT, Akita RW and Sliwkowski MX. (1999) Binding specificities and affinities of egf domains for ErbB receptors. FEBS Lett 447: 227-31 [PMID:10214951]
68. Junttila MR, Warne R, Repellin C, Sambucetti L, Chang J, Kim S, Kim HY, Shin DG, Park DH and Patel R et al.. 1345P Preclinical activity of ORIC-114, a highly selective, brain penetrant, irreversible kinase inhibitor, against atypical mutations in EGFR https://www.annalsofoncology.org/article/S0923-7534(23)03215-5/fulltext. Accessed on 05/05/2025.
69. Kammasud N, Boonyarat C, Sanphanya K, Utsintong M, Tsunoda S, Sakurai H, Saiki I, André I, Grierson DS and Vajragupta O. (2009) 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorg Med Chem Lett 19: 745-50 [PMID:19110422]
70. Kao Y-H and Vanderlaan M. (2006) Her2 antibody composition. Patent number: WO2006033700. Assignee: Genentech Inc.. Priority date: 22/07/2004. Publication date: 30/04/2010.
71. Kashima K, Kawauchi H, Tanimura H, Tachibana Y, Chiba T, Torizawa T and Sakamoto H. (2020) CH7233163 Overcomes Osimertinib-Resistant EGFR-Del19/T790M/C797S Mutation. Mol Cancer Ther 19: 2288-2297 [PMID:32943545]
72. Kaspersen SJ, Sørum C, Willassen V, Fuglseth E, Kjøbli E, Bjørkøy G, Sundby E and Hoff BH. (2011) Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines. Eur J Med Chem 46: 6002-14 [PMID:22018877]
73. Katayama R, Khan TM, Benes C, Lifshits E, Ebi H, Rivera VM, Shakespeare WC, Iafrate AJ, Engelman JA and Shaw AT. (2011) Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci USA 108: 7535-40 [PMID:21502504]
74. Kearns JD, Bukhalid R, Sevecka M, Tan G, Gerami-Moayed N, Werner SL, Kohli N, Burenkova O, Sloss CM and King AM et al.. (2015) Enhanced Targeting of the EGFR Network with MM-151, an Oligoclonal Anti-EGFR Antibody Therapeutic. Mol Cancer Ther 14: 1625-36 [PMID:25911688]
75. Kiewe P and Thiel E. (2008) Ertumaxomab: a trifunctional antibody for breast cancer treatment. Expert Opin Investig Drugs 17: 1553-8 [PMID:18808314]
76. Klutchko SR, Zhou H, Winters RT, Tran TP, Bridges AJ, Althaus IW, Amato DM, Elliott WL, Ellis PA and Meade MA et al.. (2006) Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors. J Med Chem 49: 1475-85 [PMID:16480284]
77. Kulukian A, Lee P, Taylor J, Rosler R, de Vries P, Watson D, Forero-Torres A and Peterson S. (2020) Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models. Mol Cancer Ther 19: 976-987 [PMID:32241871]
78. Lee KH, Xin R, Cui J, Cai Z, Choi HJ, Zheng M, Tian B, Zhao B, Park C, Jin H and Daugirala KB. (2020) N2, N4-diphenylpyrimidine-2, 4-diamine derivative, process for producing the same, and pharmaceutical composition for preventing or treating cancer comprising the same as active ingredient Patent number: CN110740999A. Assignee: Korea Institute Of Chemistry Korea Research Institute of Chemical Technology KRICT. Priority date: 12/06/2018. Publication date: 31/01/2020.
79. Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, Padera RF, Shapiro GI, Baum A and Himmelsbach F et al.. (2008) BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene 27: 4702-11 [PMID:18408761]
80. Li MC, Coumar MS, Lin SY, Lin YS, Huang GL, Chen CH, Lien TW, Wu YW, Chen YT and Chen CP et al.. (2023) Development of Furanopyrimidine-Based Orally Active Third-Generation EGFR Inhibitors for the Treatment of Non-Small Cell Lung Cancer. J Med Chem 66: 2566-2588 [PMID:36749735]
81. Li X, Yang C, Wan H, Zhang G, Feng J, Zhang L, Chen X, Zhong D, Lou L and Tao W et al.. (2017) Discovery and development of pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer. Eur J Pharm Sci 110: 51-61 [PMID:28115222]
82. Li X, Zuo Y, Tang G, Wang Y, Zhou Y, Wang X, Guo T, Xia M, Ding N and Pan Z. (2014) Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. J Med Chem 57: 5112-28 [PMID:24915291]
83. Li Z, Zou H, Zhu W, Shen C, Wang R, Liu W, Chen X, Tsui H, Yang Z and Zhang X. (2019) Erbb/btk inhibitors Patent number: WO2019149164A1. Assignee: Dizal (Jiangsu) Pharmaceutical Co., Ltd. Priority date: 31/01/2018. Publication date: 08/09/2019.
84. Lim SM, Xie T, Westover KD, Ficarro SB, Tae HS, Gurbani D, Sim T, Marto JA, Jänne PA and Crews CM et al.. (2015) Development of small molecules targeting the pseudokinase Her3. Bioorg Med Chem Lett 25: 3382-9 [PMID:26094118]
85. Lin SY, Chang Hsu Y, Peng YH, Ke YY, Lin WH, Sun HY, Shiao HY, Kuo FM, Chen PY and Lien TW et al.. (2019) Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. J Med Chem 62: 10108-10123 [PMID:31560541]
86. Liu B, Gao F, Zhao H, Yuan S, Peng X, Zhang P, Wang J, Zhang T, Duan M and Guo Y. (2023) Discovery of YK-029A, a novel mutant EGFR inhibitor targeting both T790 M and exon 20 insertion mutations, as a treatment for NSCLC. Eur J Med Chem 258: 115590 [PMID:37406381]
87. Liu M and Zhu Z. (2009) Used in treating neoplastic diseases and hyperproliferative disorders. Patent number: US7598350. Assignee: Imclone Llc. Priority date: 19/03/2004. Publication date: 06/10/2009.
88. Lu X, Zhang T, Zhu SJ, Xun Q, Tong L, Hu X, Li Y, Chan S, Su Y and Sun Y et al.. (2018) Discovery of JND3229 as a New EGFR^C797S Mutant Inhibitor with In Vivo Monodrug Efficacy. ACS Med Chem Lett 9: 1123-1127 [PMID:30429956]
89. Lucas MC, Padilla F, Flohr A, Arista L and Buck E. (2021) Alkynyl quinazoline compounds Patent number: WO2021030711A1. Assignee: Black Diamond Therapeutics. Priority date: 14/08/2020. Publication date: 18/02/2021.
90. Luo H, Zhou H, Wang S and Wu Y. (2018) Pyridinylaminopyrimidine derivatives, preparation process and use thereof. Patent number: US10072002B2. Assignee: Shanghai Allist Pharmaceuticals Inc. Priority date: 21/04/2015. Publication date: 11/09/2018.
91. Mao L, Pan W, Wang X, Zhang Y, Li R, Waykole L and Sethuraman V. (2015) Egfr inhibitor forms Patent number: WO2015085482. Assignee: Novartis Ag. Priority date: 10/12/2013. Publication date: 18/06/2015.
92. Marathe P, Tang Y, Sleczka B, Rodrigues D, Gavai A, Wong T, Christopher L and Zhang H. (2010) Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci 99: 3579-93 [PMID:20166197]
93. Matsuya T, Kondoh Y, Shimada I, Kikuchi S, Iida M, Onda K, Fukudome H, Takemoto Y, Shindou N, Sakagami H and Hamaguchi H. (2013) Pyrazine carboxamide compound Patent number: WO2013108754. Assignee: Astellas Pharma Inc.. Priority date: 17/01/2012. Publication date: 25/07/2013.
94. McDonagh CF, Huhalov A, Harms BD, Adams S, Paragas V, Oyama S, Zhang B, Luus L, Overland R and Nguyen S et al.. (2012) Antitumor activity of a novel bispecific antibody that targets the ErbB2/ErbB3 oncogenic unit and inhibits heregulin-induced activation of ErbB3. Mol Cancer Ther 11: 582-93 [PMID:22248472]
95. Meng Y, Yu B, Huang H, Peng Y, Li E, Yao Y, Song C, Yu W, Zhu K and Wang K et al.. (2021) Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. J Med Chem 64: 925-937 [PMID:33459024]
96. Nagasawa J, Mizokami A, Koshida K, Yoshida S, Naito K and Namiki M. (2006) Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int J Urol 13: 587-92 [PMID:16771730]
97. Nam HJ, Kim HP, Yoon YK, Hur HS, Song SH, Kim MS, Lee GS, Han SW, Im SA and Kim TY et al.. (2011) Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer. Cancer Lett 302: 155-65 [PMID:21306821]
98. Obst-Sander U, Ricci A, Kuhn B, Friess T, Koldewey P, Kuglstatter A, Hewings D, Goergler A, Steiner S and Rueher D et al.. (2022) Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. J Med Chem 65: 13052-13073 [PMID:36178776]
99. Ogiso H, Ishitani R, Nureki O, Fukai S, Yamanaka M, Kim JH, Saito K, Sakamoto A, Inoue M and Shirouzu M et al.. (2002) Crystal structure of the complex of human epidermal growth factor and receptor extracellular domains. Cell 110: 775-87 [PMID:12297050]
100. Onoda T, Iinuma H, Sasaki Y, Hamada M, Isshiki K, Naganawa H, Takeuchi T, Tatsuta K and Umezawa K. (1989) Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus. J Nat Prod 52: 1252-7 [PMID:2614420]
101. Pagliarini RA, Milgram BC, Borrelli DR, O'Hearn E, Huff MR, Ladd B, Brooijmans N, Wang W, Kuzmic P and Guzman-Perez A et al.. (2023) Abstract B168: Identification of STX-241, a CNS-penetrant and mutant-selective EGFR inhibitor with activity on osimertinib-resistant C797x mutations Mol Cancer Ther 22
102. Panek RL, Lu GH, Klutchko SR, Batley BL, Dahring TK, Hamby JM, Hallak H, Doherty AM and Keiser JA. (1997) In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor. J Pharmacol Exp Ther 283: 1433-44 [PMID:9400019]
103. Park JK, Byun JY, Park JA, Kim YY, Lee YJ, Oh JI, Jang SY, Kim YH, Song YW and Son J et al.. (2015) HM71224, a novel Bruton's tyrosine kinase inhibitor, suppresses B cell and monocyte activation and ameliorates arthritis in a mouse model: a potential drug for rheumatoid arthritis. Arthritis Res Ther 18: 91 [PMID:27090981]
104. Patel H, Pawara R, Ansari A and Surana S. (2017) Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance. Eur J Med Chem 142: 32-47 [PMID:28526474]
105. Peng J, Costanzo MJ, Greco MN, Green MA, Wilde VL and Zhang D. (2016) Substituted 2-anilinopyrimidine derivatives as EGFR modulators Patent number: WO2016094821A2. Assignee: Beta Pharma, Inc.. Priority date: 11/12/2014. Publication date: 16/06/2016.
106. Phillips RM. (2016) Targeting the hypoxic fraction of tumours using hypoxia-activated prodrugs. Cancer Chemother Pharmacol 77: 441-57 [PMID:26811177]
107. Planken S, Behenna DC, Nair SK, Johnson TO, Nagata A, Almaden C, Bailey S, Ballard TE, Bernier L and Cheng H et al.. (2017) Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR. J Med Chem 60: 3002-3019 [PMID:28287730]
108. Qi B, Yang Y, Gong G, He H, Yue X, Xu X, Hu Y, Li J, Chen T and Wan X et al.. (2019) Discovery of N¹-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)-N³-(2-(2,6-difluorophenyl)-4-oxothiazolidin-3-yl)urea as a multi-tyrosine kinase inhibitor for drug-sensitive and drug-resistant cancers treatment. Eur J Med Chem 163: 10-27 [PMID:30503936]
109. Qiu C, Tarrant MK, Choi SH, Sathyamurthy A, Bose R, Banjade S, Pal A, Bornmann WG, Lemmon MA and Cole PA et al.. (2008) Mechanism of activation and inhibition of the HER4/ErbB4 kinase. Structure 16: 460-7 [PMID:18334220]
110. Rabindran SK, Discafani CM, Rosfjord EC, Baxter M, Floyd MB, Golas J, Hallett WA, Johnson BD, Nilakantan R and Overbeek E et al.. (2004) Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res 64: 3958-65 [PMID:15173008]
111. Ren Y, Zheng J, Fan S, Wang L, Cheng M, Shi D, Zhang W, Tang R, Yu Y and Jiao L et al.. (2017) Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget 8: 50832-50844 [PMID:28881608]
112. Rewcastle GW, Bridges AJ, Fry DW, Rubin JR and Denny WA. (1997) Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor. J Med Chem 40: 1820-6 [PMID:9191958]
113. Rewcastle GW, Palmer BD, Bridges AJ, Showalter HD, Sun L, Nelson J, McMichael A, Kraker AJ, Fry DW and Denny WA. (1996) Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor. J Med Chem 39: 918-28 [PMID:8632415]
114. Romagnoli R, Prencipe F, Oliva P, Baraldi S, Baraldi PG, Schiaffino Ortega S, Chayah M, Kimatrai Salvador M, Lopez-Cara LC and Brancale A et al.. (2019) Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors. J Med Chem 62: 1274-1290 [PMID:30633509]
115. Rusnak DW, Lackey K, Affleck K, Wood ER, Alligood KJ, Rhodes N, Keith BR, Murray DM, Knight WB and Mullin RJ et al.. (2001) The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther 1: 85-94 [PMID:12467226]
116. Schoeberl B, Pace EA, Fitzgerald JB, Harms BD, Xu L, Nie L, Linggi B, Kalra A, Paragas V and Bukhalid R et al.. (2009) Therapeutically targeting ErbB3: a key node in ligand-induced activation of the ErbB receptor-PI3K axis. Sci Signal 2: ra31 [PMID:19567914]
117. Shi F, Telesco SE, Liu Y, Radhakrishnan R and Lemmon MA. (2010) ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylation. Proc Natl Acad Sci USA 107: 7692-7 [PMID:20351256]
118. Smaill JB, Rewcastle GW, Loo JA, Greis KD, Chan OH, Reyner EL, Lipka E, Showalter HD, Vincent PW and Elliott WL et al.. (2000) Tyrosine kinase inhibitors. 17. 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. J Med Chem 43: 1380-97 [PMID:10753475]
119. Solca FF, Baum A, Langkopf E, Dahmann G, Heider KH, Himmelsbach F and van Meel JC. (2004) Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J Pharmacol Exp Ther 311: 502-9 [PMID:15199094]
120. Suh B-C, Salgaonkar PD, Lee J, Koh JS, Song H-J, Lee IY, Lee J, Jung DS, Kim J-H and Kim S-W. (2016) Compounds and compositions for modulating EGFR mutant kinase activities. Patent number: WO2016060443A2. Assignee: Yuhan Corporation. Priority date: 13/10/2014. Publication date: 21/04/2016.
121. Tang Z, Yuan X, Du R, Cheung SH, Zhang G, Wei J, Zhao Y, Feng Y, Peng H and Zhang Y et al.. (2015) BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol Cancer Ther 14: 2187-97 [PMID:26208524]
122. To C, Beyett TS, Jang J, Feng WW, Bahcall M, Haikala HM, Shin BH, Heppner DE, Rana JK and Leeper BA et al.. (2022) An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nat Cancer 3: 402-417 [PMID:35422503]
123. To C, Jang J, Chen T, Park E, Mushajiang M, De Clercq DJH, Xu M, Wang S, Cameron MD and Heppner DE et al.. (2019) Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov 9: 926-943 [PMID:31092401]
124. Traxler P, Allegrini PR, Brandt R, Brueggen J, Cozens R, Fabbro D, Grosios K, Lane HA, McSheehy P and Mestan J et al.. (2004) AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res 64: 4931-41 [PMID:15256466]
125. Traxler P, Green J, Mett H, Séquin U and Furet P. (1999) Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones. J Med Chem 42: 1018-26 [PMID:10090785]
126. Trudel S, Li ZH, Wei E, Wiesmann M, Chang H, Chen C, Reece D, Heise C and Stewart AK. (2005) CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood 105: 2941-8 [PMID:15598814]
127. Tzahar E, Pinkas-Kramarski R, Moyer JD, Klapper LN, Alroy I, Levkowitz G, Shelly M, Henis S, Eisenstein M and Ratzkin BJ et al.. (1997) Bivalence of EGF-like ligands drives the ErbB signaling network. EMBO J 16: 4938-50 [PMID:9305636]
128. Uddin M, Lau LC, Seumois G, Vijayanand P, Staples KJ, Bagmane D, Cornelius V, Dorinsky P, Davies DE and Djukanović R. (2013) EGF-induced bronchial epithelial cells drive neutrophil chemotactic and anti-apoptotic activity in asthma. PLoS ONE 8: e72502 [PMID:24039773]
129. Walter AO, Sjin RT, Haringsma HJ, Ohashi K, Sun J, Lee K, Dubrovskiy A, Labenski M, Zhu Z and Wang Z et al.. (2013) Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov 3: 1404-15 [PMID:24065731]
130. Wang S, Cang S and Liu D. (2016) Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. J Hematol Oncol 9: 34 [PMID:27071706]
131. Wei R, Zhang W, Yang F, Li Q, Wang Q, Liu N, Zhu J and Shan Y. (2024) Dual targeting non-overlapping epitopes in HER2 domain IV substantially enhanced HER2/HER2 homodimers and HER2/EGFR heterodimers internalization leading to potent antitumor activity in HER2-positive human gastric cancer. J Transl Med 22: 641 [PMID:38982548]
132. Wilding B, Boese D, Engelhardt H, Fuchs J, Neumueller R, Petronczki M, Scham D and Treu M. (2021) [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors Patent number: WO2021156178A1. Assignee: Boehringer Ingelheim International Gmbh. Priority date: 03/02/2020. Publication date: 12/08/2021.
133. Wilding B, Scharn D, Böse D, Baum A, Santoro V, Chetta P, Schnitzer R, Botesteanu DA, Reiser C and Kornigg S et al.. (2022) Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling. Nat Cancer 3: 821-836 [PMID:35883003]
134. Wissner A, Fraser HL, Ingalls CL, Dushin RG, Floyd MB, Cheung K, Nittoli T, Ravi MR, Tan X and Loganzo F. (2007) Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. Bioorg Med Chem 15: 3635-48 [PMID:17416531]
135. Wissner A, Hamann PR, Nilakantan R, Greenberger LM, Ye F, Rapuano TA and Loganzo F. (2004) Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles. Bioorg Med Chem Lett 14: 1411-6 [PMID:15006373]
136. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC and Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol 17: 1241-9 [PMID:21095574]
137. Wood ER, Shewchuk LM, Ellis B, Brignola P, Brashear RL, Caferro TR, Dickerson SH, Dickson HD, Donaldson KH and Gaul M et al.. (2008) 6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases. Proc Natl Acad Sci USA 105: 2773-8 [PMID:18287036]
138. Wood ER, Truesdale AT, McDonald OB, Yuan D, Hassell A, Dickerson SH, Ellis B, Pennisi C, Horne E and Lackey K et al.. (2004) A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res 64: 6652-9 [PMID:15374980]
139. Wu L, Liu X, Ding CZ, Chen S, Hu L, Zhao L, Pan W, Hu G, Li J and Zhao N et al.. (2019) Aryl-phosphorus-oxygen compound as egfr kinase inhibitor Patent number: WO2019015655A1. Assignee: Chia Tai Tianqing Pharmaceutical Group Co Ltd. Priority date: 19/07/2018. Publication date: 24/01/2019.
140. Xie H, Lin L, Tong L, Jiang Y, Zheng M, Chen Z, Jiang X, Zhang X, Ren X and Qu W et al.. (2011) AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS ONE 6: e21487 [PMID:21789172]
141. Xu X, Mao L, Xu W, Tang W, Zhang X, Xi B, Xu R, Fang X, Liu J and Fang C et al.. (2016) AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients. Mol Cancer Ther 15: 2586-2597 [PMID:27573423]
142. Yamamoto F, Mizutani T, Kasuga H, Fuchida Y, Hara S, Kobayakawa Y and Ogino E. (2020) 7h-pyrrolo[2,3-d]pyrimidine-4-amine derivative Patent number: WO2020166680A1. Assignee: Taiho Pharmaceutical Co., Ltd.. Priority date: 14/02/2020. Publication date: 20/08/2020.
143. Yang Z, Liu Z, Wan S, Xu J, Huang Y, He H, Liu T, Li L, Ren Y and Zhang J et al.. (2024) Discovery of Novel Small-Molecule-Based Potential PD-L1/EGFR Dual Inhibitors with High Druggability for Glioblastoma Immunotherapy. J Med Chem 67: 7995-8019 [PMID:38739112]
144. Yin J and Tao J. (2013) Aminoquinazoline derivative and use thereof in preparing anti-malignant tumor medicament Patent number: WO2013135176A1. Assignee: Suzhou Maitai Biotechnology Co., Ltd.. Priority date: 16/03/2012. Publication date: 19/09/2013.
145. Yu H, Wei M, Cui Y, Sun X, Tong C, Sun G, Tan S, Ma J, Gao P and Liao J et al.. (2016) Egfr inhibitor, and preparation and application thereof Patent number: WO2016054987A1. Assignee: Shanghai Hansen Biomedical Technology Co, Jiangsu Hansen Pharmaceutical Group Co. Priority date: 11/10/2014. Publication date: 14/04/2016.
146. Zeng Q, Wang J, Cheng Z, Chen K, Johnström P, Varnäs K, Li DY, Yang ZF and Zhang X. (2015) Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem 58: 8200-15 [PMID:26313252]
147. Zhang L, Fan C, Guo Z, Li Y, Zhao S, Yang S, Yang Y, Zhu J and Lin D. (2013) Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer. Eur J Med Chem 69: 833-41 [PMID:24121234]
148. Zhang T, Qu R, Chan S, Lai M, Tong L, Feng F, Chen H, Song T, Song P and Bai G et al.. (2020) Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer 19: 90 [PMID:32404161]
149. Zhang YM, Cockerill S, Guntrip SB, Rusnak D, Smith K, Vanderwall D, Wood E and Lackey K. (2004) Synthesis and SAR of potent EGFR/erbB2 dual inhibitors. Bioorg Med Chem Lett 14: 111-4 [PMID:14684309]
150. Zhou D and Cheng Z. (2020) Quinazoline derivatives as antitumor agents Patent number: WO2020057511A1. Assignee: Suzhou Zanrong Pharma Limited. Priority date: 19/02/2019. Publication date: 26/03/2020.
151. Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE and Padera R et al.. (2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462: 1070-4 [PMID:20033049]
152. Zhu X, Jiang M and Ji A. (2019) 2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof Patent number: US10414756B2. Assignee: Nanjing Diansu Biological Technology Co Ltd. Priority date: 31/07/2015. Publication date: 17/09/2019.
153. Zhu Y, Ye X, Shen H, Li J, Cai Z, Min W, Hou W, Dong H, Wu Y and Wang L et al.. (2023) Discovery of Novel Fourth-Generation EGFR Inhibitors to Overcome C797S-Mediated Resistance J Med Chem