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Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation.
Hennessy EJ, Chuaqui C, Ashton S, Colclough N, Cross DA, Debreczeni JÉ, Eberlein C, Gingipalli L, Klinowska TC, Orme JP, Sha L, Wu X. Hennessy EJ, et al. Among authors: klinowska tc. ACS Med Chem Lett. 2016 Mar 21;7(5):514-9. doi: 10.1021/acsmedchemlett.6b00058. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190603 Free PMC article.
Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.
Ballard P, Bradbury RH, Harris CS, Hennequin LF, Hickinson M, Johnson PD, Kettle JG, Klinowska T, Leach AG, Morgentin R, Pass M, Ogilvie DJ, Olivier A, Warin N, Williams EJ. Ballard P, et al. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1633-7. doi: 10.1016/j.bmcl.2005.12.028. Epub 2005 Dec 27. Bioorg Med Chem Lett. 2006. PMID: 16380259
Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Barlaam B, Acton DG, Ballard P, Bradbury RH, Cross D, Ducray R, Germain H, Hudson K, Klinowska T, Magnien F, Ogilvie DJ, Olivier A, Ross HS, Smith R, Trigwell CB, Vautier M, Wright L. Barlaam B, et al. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1799-803. doi: 10.1016/j.bmcl.2008.02.035. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18313293
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Ward RA, Anderton MJ, Ashton S, Bethel PA, Box M, Butterworth S, Colclough N, Chorley CG, Chuaqui C, Cross DA, Dakin LA, Debreczeni JÉ, Eberlein C, Finlay MR, Hill GB, Grist M, Klinowska TC, Lane C, Martin S, Orme JP, Smith P, Wang F, Waring MJ. Ward RA, et al. Among authors: klinowska tc. J Med Chem. 2013 Sep 12;56(17):7025-48. doi: 10.1021/jm400822z. Epub 2013 Aug 30. J Med Chem. 2013. PMID: 23930994
AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA, Mellor MJ, Hughes G, Rahi A, Jacobs VN, Red Brewer M, Ichihara E, Sun J, Jin H, Ballard P, Al-Kadhimi K, Rowlinson R, Klinowska T, Richmond GH, Cantarini M, Kim DW, Ranson MR, Pao W. Cross DA, et al. Cancer Discov. 2014 Sep;4(9):1046-61. doi: 10.1158/2159-8290.CD-14-0337. Epub 2014 Jun 3. Cancer Discov. 2014. PMID: 24893891 Free PMC article.
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.
Finlay MR, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DA, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL. Finlay MR, et al. J Med Chem. 2014 Oct 23;57(20):8249-67. doi: 10.1021/jm500973a. Epub 2014 Oct 1. J Med Chem. 2014. PMID: 25271963
46 results