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Page 1
The Next-Generation Oral Selective Estrogen Receptor Degrader Camizestrant (AZD9833) Suppresses ER+ Breast Cancer Growth and Overcomes Endocrine and CDK4/6 Inhibitor Resistance.
Lawson M, Cureton N, Ros S, Cheraghchi-Bashi A, Urosevic J, D'Arcy S, Delpuech O, DuPont M, Fisher DI, Gangl ET, Lewis H, Trueman D, Wali N, Williamson SC, Moss J, Montaudon E, Derrien H, Marangoni E, Miragaia RJ, Gagrica S, Morentin-Gutierrez P, Moss TA, Maglennon G, Sutton D, Polanski R, Rosen A, Cairns J, Zhang P, Sánchez-Guixé M, Serra V, Critchlow SE, Scott JS, Lindemann JPO, Barry ST, Klinowska T, Morrow CJ, Carnevalli LS. Lawson M, et al. Among authors: scott js. Cancer Res. 2023 Dec 1;83(23):3989-4004. doi: 10.1158/0008-5472.CAN-23-0694. Cancer Res. 2023. PMID: 37725704 Free PMC article.
Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.
Scott JS, Bailey A, Buttar D, Carbajo RJ, Curwen J, Davey PRJ, Davies RDM, Degorce SL, Donald C, Gangl E, Greenwood R, Groombridge SD, Johnson T, Lamont S, Lawson M, Lister A, Morrow CJ, Moss TA, Pink JH, Polanski R. Scott JS, et al. J Med Chem. 2019 Feb 14;62(3):1593-1608. doi: 10.1021/acs.jmedchem.8b01837. Epub 2019 Jan 30. J Med Chem. 2019. PMID: 30640465
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Scott JS, Moss TA, Balazs A, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Davey PRJ, Delpuech O, Fawell S, Fisher DI, Gagrica S, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Herlihy K, Hughes S, Hunt TA, Huynh H, Janbon SLM, Johnson T, Kavanagh S, Klinowska T, Lawson M, Lister AS, Marden S, McGinnity DF, Morrow CJ, Nissink JWM, O'Donovan DH, Peng B, Polanski R, Stead DS, Stokes S, Thakur K, Throner SR, Tucker MJ, Varnes J, Wang H, Wilson DM, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. J Med Chem. 2020 Dec 10;63(23):14530-14559. doi: 10.1021/acs.jmedchem.0c01163. Epub 2020 Sep 29. J Med Chem. 2020. PMID: 32910656
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.
Scott JS, Moss TA, Barlaam B, Davey PRJ, Fairley G, Gangl ET, Greenwood RDR, Hatoum-Mokdad H, Lister AS, Longmire D, Polanski R, Stokes S, Tucker MJ, Varnes JG, Yang B. Scott JS, et al. ACS Med Chem Lett. 2020 Oct 28;11(12):2519-2525. doi: 10.1021/acsmedchemlett.0c00505. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335676 Free PMC article.
Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.
Scott JS, Stead D, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Cureton N, Davey PRJ, Fisher DI, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Hughes SJ, Hunt TA, Johnson T, Kavanagh SL, Klinowska TCM, Larner CJB, Lawson M, Lister AS, Longmire D, Marden S, McGuire TM, McMillan C, McMurray L, Morrow CJ, Nissink JWM, Moss TA, O'Donovan DH, Polanski R, Stokes S, Thakur K, Trueman D, Truman C, Tucker MJ, Wang H, Whalley N, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. J Med Chem. 2023 Feb 23;66(4):2918-2945. doi: 10.1021/acs.jmedchem.2c01964. Epub 2023 Feb 1. J Med Chem. 2023. PMID: 36727211
Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC.
Hayhow TG, Williamson B, Lawson M, Cureton N, Braybrooke EL, Campbell A, Carbajo RJ, Cheraghchi-Bashi A, Chiarparin E, Diène CR, Fallan C, Fisher DI, Goldberg FW, Hopcroft L, Hopcroft P, Jackson A, Kettle JG, Klinowska T, Künzel U, Lamont G, Lewis HJ, Maglennon G, Martin S, Gutierrez PM, Morrow CJ, Nikolaou M, Nissink JWM, O'Shea P, Polanski R, Schade M, Scott JS, Smith A, Weber J, Wilson J, Yang B, Crafter C. Hayhow TG, et al. Among authors: scott js. Commun Biol. 2024 May 13;7(1):563. doi: 10.1038/s42003-024-06238-x. Commun Biol. 2024. PMID: 38740899 Free PMC article.
Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Ballard P, Barlaam BC, Bradbury RH, Dishington A, Hennequin LF, Hickinson DM, Hollingsworth IM, Kettle JG, Klinowska T, Ogilvie DJ, Pearson SE, Scott JS, Suleman A, Whittaker R, Williams EJ, Wood R, Wright L. Ballard P, et al. Among authors: scott js. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6326-9. doi: 10.1016/j.bmcl.2007.08.073. Epub 2007 Sep 2. Bioorg Med Chem Lett. 2007. PMID: 17869514
411 results