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Items: 1 to 20 of 124

1.

QSAR-based models for designing quinazoline/imidazothiazoles/pyrazolopyrimidines based inhibitors against wild and mutant EGFR.

Chauhan JS, Dhanda SK, Singla D; Open Source Drug Discovery Consortium, Agarwal SM, Raghava GP.

PLoS One. 2014 Jul 3;9(7):e101079. doi: 10.1371/journal.pone.0101079. eCollection 2014.

2.

QSAR based model for discriminating EGFR inhibitors and non-inhibitors using Random forest.

Singh H, Singh S, Singla D, Agarwal SM, Raghava GP.

Biol Direct. 2015 Mar 25;10:10. doi: 10.1186/s13062-015-0046-9.

3.

Homology models of the mutated EGFR and their response towards quinazoline analogues.

Kotra S, Madala KK, Jamil K.

J Mol Graph Model. 2008 Oct;27(3):244-54. doi: 10.1016/j.jmgm.2008.04.010. Epub 2008 May 3.

PMID:
18585943
4.

Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library.

Zhang Q, Liu Y, Gao F, Ding Q, Cho C, Hur W, Jin Y, Uno T, Joazeiro CA, Gray N.

J Am Chem Soc. 2006 Feb 22;128(7):2182-3.

PMID:
16478150
6.

Synthesis and characterization of novel quinazoline type inhibitors for mutant and wild-type EGFR and RICK kinases.

Breza N, Pato J, Orfi L, Hegymegi-Barakonyi B, Banhegyi P, Varkondi E, Borbely G, Petak I, Keri G.

J Recept Signal Transduct Res. 2008;28(4):361-73. doi: 10.1080/10799890802242618 .

PMID:
18702009
7.

Combined therapy with mutant-selective EGFR inhibitor and Met kinase inhibitor for overcoming erlotinib resistance in EGFR-mutant lung cancer.

Nakagawa T, Takeuchi S, Yamada T, Nanjo S, Ishikawa D, Sano T, Kita K, Nakamura T, Matsumoto K, Suda K, Mitsudomi T, Sekido Y, Uenaka T, Yano S.

Mol Cancer Ther. 2012 Oct;11(10):2149-57. doi: 10.1158/1535-7163.MCT-12-0195. Epub 2012 Jul 25.

8.

Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.

Michalczyk A, Klüter S, Rode HB, Simard JR, Grütter C, Rabiller M, Rauh D.

Bioorg Med Chem. 2008 Apr 1;16(7):3482-8. doi: 10.1016/j.bmc.2008.02.053. Epub 2008 Feb 20.

PMID:
18316192
9.

6-Aryl and heterocycle quinazoline derivatives as potent EGFR inhibitors with improved activity toward gefitinib-sensitive and -resistant tumor cell lines.

Hamed MM, Abou El Ella DA, Keeton AB, Piazza GA, Abadi AH, Hartmann RW, Engel M.

ChemMedChem. 2013 Sep;8(9):1495-504. doi: 10.1002/cmdc.201300147. Epub 2013 Jul 11.

PMID:
23847159
10.

Noncovalent wild-type-sparing inhibitors of EGFR T790M.

Lee HJ, Schaefer G, Heffron TP, Shao L, Ye X, Sideris S, Malek S, Chan E, Merchant M, La H, Ubhayakar S, Yauch RL, Pirazzoli V, Politi K, Settleman J.

Cancer Discov. 2013 Feb;3(2):168-81. doi: 10.1158/2159-8290.CD-12-0357. Epub 2012 Dec 10.

11.

3D-QSAR and molecular docking studies of 4-anilinoquinazoline derivatives: a rational approach to anticancer drug design.

Nandi S, Bagchi MC.

Mol Divers. 2010 Feb;14(1):27-38. doi: 10.1007/s11030-009-9137-9. Epub 2009 Mar 28.

PMID:
19330460
12.

Novel 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors.

Barbosa ML, Lima LM, Tesch R, Sant'Anna CM, Totzke F, Kubbutat MH, Schächtele C, Laufer SA, Barreiro EJ.

Eur J Med Chem. 2014 Jan;71:1-14. doi: 10.1016/j.ejmech.2013.10.058. Epub 2013 Oct 31.

PMID:
24269511
13.

Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation.

Sos ML, Rode HB, Heynck S, Peifer M, Fischer F, Klüter S, Pawar VG, Reuter C, Heuckmann JM, Weiss J, Ruddigkeit L, Rabiller M, Koker M, Simard JR, Getlik M, Yuza Y, Chen TH, Greulich H, Thomas RK, Rauh D.

Cancer Res. 2010 Feb 1;70(3):868-74. doi: 10.1158/0008-5472.CAN-09-3106. Epub 2010 Jan 26.

14.

QSAR of aromatic substances: EGFR inhibitory activity of quinazoline analogues.

Deeb O, Clare BW.

J Enzyme Inhib Med Chem. 2008 Dec;23(6):763-75. doi: 10.1080/14756360701608726 .

PMID:
18608750
15.

Structural investigations of T854A mutation in EGFR and identification of novel inhibitors using structure activity relationships.

Goyal S, Jamal S, Shanker A, Grover A.

BMC Genomics. 2015;16 Suppl 5:S8. doi: 10.1186/1471-2164-16-S5-S8. Epub 2015 May 26.

16.

Discovery of 6-substituted 4-anilinoquinazolines with dioxygenated rings as novel EGFR tyrosine kinase inhibitors.

Li DD, Fang F, Li JR, Du QR, Sun J, Gong HB, Zhu HL.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5870-5. doi: 10.1016/j.bmcl.2012.07.079. Epub 2012 Jul 31.

PMID:
22901387
17.

Discovery of pteridin-7(8H)-one-based irreversible inhibitors targeting the epidermal growth factor receptor (EGFR) kinase T790M/L858R mutant.

Zhou W, Liu X, Tu Z, Zhang L, Ku X, Bai F, Zhao Z, Xu Y, Ding K, Li H.

J Med Chem. 2013 Oct 24;56(20):7821-37. doi: 10.1021/jm401045n. Epub 2013 Oct 9.

PMID:
24053674
18.

A comparative QSAR analysis of quinazoline analogues as tyrosine kinase (erbB-2) inhibitors.

Noolvi MN, Patel HM, Bhardwaj V.

Med Chem. 2011 May;7(3):200-12. doi: 1573-4064/11 $58.00+.00.

PMID:
21486203
19.

Novel oxazolo[4,5-g]quinazolin-2(1H)-ones: dual inhibitors of EGFR and Src protein tyrosine kinases.

Lin J, Shen W, Xue J, Sun J, Zhang X, Zhang C.

Eur J Med Chem. 2012 Sep;55:39-48. doi: 10.1016/j.ejmech.2012.06.055. Epub 2012 Jul 7.

PMID:
22818848
20.

AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo.

Xie H, Lin L, Tong L, Jiang Y, Zheng M, Chen Z, Jiang X, Zhang X, Ren X, Qu W, Yang Y, Wan H, Chen Y, Zuo J, Jiang H, Geng M, Ding J.

PLoS One. 2011;6(7):e21487. doi: 10.1371/journal.pone.0021487. Epub 2011 Jul 18.

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