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Page 1
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
De Savi C, Bradbury RH, Rabow AA, Norman RA, de Almeida C, Andrews DM, Ballard P, Buttar D, Callis RJ, Currie GS, Curwen JO, Davies CD, Donald CS, Feron LJ, Gingell H, Glossop SC, Hayter BR, Hussain S, Karoutchi G, Lamont SG, MacFaul P, Moss TA, Pearson SE, Tonge M, Walker GE, Weir HM, Wilson Z. De Savi C, et al. Among authors: weir hm. J Med Chem. 2015 Oct 22;58(20):8128-40. doi: 10.1021/acs.jmedchem.5b00984. Epub 2015 Oct 7. J Med Chem. 2015. PMID: 26407012
AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models.
Weir HM, Bradbury RH, Lawson M, Rabow AA, Buttar D, Callis RJ, Curwen JO, de Almeida C, Ballard P, Hulse M, Donald CS, Feron LJ, Karoutchi G, MacFaul P, Moss T, Norman RA, Pearson SE, Tonge M, Davies G, Walker GE, Wilson Z, Rowlinson R, Powell S, Sadler C, Richmond G, Ladd B, Pazolli E, Mazzola AM, D'Cruz C, De Savi C. Weir HM, et al. Cancer Res. 2016 Jun 1;76(11):3307-18. doi: 10.1158/0008-5472.CAN-15-2357. Epub 2016 Mar 28. Cancer Res. 2016. PMID: 27020862
Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode.
Finlay MR, Acton DG, Andrews DM, Barker AJ, Dennis M, Fisher E, Graham MA, Green CP, Heaton DW, Karoutchi G, Loddick SA, Morgentin R, Roberts A, Tucker JA, Weir HM. Finlay MR, et al. Among authors: weir hm. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4442-6. doi: 10.1016/j.bmcl.2008.06.027. Epub 2008 Jun 12. Bioorg Med Chem Lett. 2008. PMID: 18617397
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.
Anderson M, Andrews DM, Barker AJ, Brassington CA, Breed J, Byth KF, Culshaw JD, Finlay MR, Fisher E, McMiken HH, Green CP, Heaton DW, Nash IA, Newcombe NJ, Oakes SE, Pauptit RA, Roberts A, Stanway JJ, Thomas AP, Tucker JA, Walker M, Weir HM. Anderson M, et al. Among authors: weir hm. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5487-92. doi: 10.1016/j.bmcl.2008.09.024. Epub 2008 Sep 10. Bioorg Med Chem Lett. 2008. PMID: 18815031
Activating ESR1 Mutations Differentially Affect the Efficacy of ER Antagonists.
Toy W, Weir H, Razavi P, Lawson M, Goeppert AU, Mazzola AM, Smith A, Wilson J, Morrow C, Wong WL, De Stanchina E, Carlson KE, Martin TS, Uddin S, Li Z, Fanning S, Katzenellenbogen JA, Greene G, Baselga J, Chandarlapaty S. Toy W, et al. Cancer Discov. 2017 Mar;7(3):277-287. doi: 10.1158/2159-8290.CD-15-1523. Epub 2016 Dec 16. Cancer Discov. 2017. PMID: 27986707 Free PMC article.
The oral selective oestrogen receptor degrader (SERD) AZD9496 is comparable to fulvestrant in antagonising ER and circumventing endocrine resistance.
Nardone A, Weir H, Delpuech O, Brown H, De Angelis C, Cataldo ML, Fu X, Shea MJ, Mitchell T, Veeraraghavan J, Nagi C, Pilling M, Rimawi MF, Trivedi M, Hilsenbeck SG, Chamness GC, Jeselsohn R, Osborne CK, Schiff R. Nardone A, et al. Br J Cancer. 2019 Feb;120(3):331-339. doi: 10.1038/s41416-018-0354-9. Epub 2018 Dec 17. Br J Cancer. 2019. PMID: 30555156 Free PMC article.
Effective combination therapies in preclinical endocrine resistant breast cancer models harboring ER mutations.
Ladd B, Mazzola AM, Bihani T, Lai Z, Bradford J, Collins M, Barry E, Goeppert AU, Weir HM, Hearne K, Renshaw JG, Mohseni M, Hurt E, Jalla S, Bao H, Hollingsworth R, Reimer C, Zinda M, Fawell S, D'Cruz CM. Ladd B, et al. Among authors: weir hm. Oncotarget. 2016 Aug 23;7(34):54120-54136. doi: 10.18632/oncotarget.10852. Oncotarget. 2016. PMID: 27472462 Free PMC article.
23 results