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Page 1
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. Among authors: gangl et. 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
Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: identification of the cycloalkylcarboxylic acids.
LaMarche MJ, Leeds JA, Amaral K, Brewer JT, Bushell SM, Dewhurst JM, Dzink-Fox J, Gangl E, Goldovitz J, Jain A, Mullin S, Neckermann G, Osborne C, Palestrant D, Patane MA, Rann EM, Sachdeva M, Shao J, Tiamfook S, Whitehead L, Yu D. LaMarche MJ, et al. J Med Chem. 2011 Dec 8;54(23):8099-109. doi: 10.1021/jm200938f. Epub 2011 Nov 1. J Med Chem. 2011. PMID: 21999529
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. J Med Chem. 2017 May 25;60(10):4386-4402. doi: 10.1021/acs.jmedchem.7b00359. Epub 2017 May 9. J Med Chem. 2017. PMID: 28485934
Correction to Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. J Med Chem. 2017 Jul 27;60(14):6459. doi: 10.1021/acs.jmedchem.7b00962. Epub 2017 Jul 17. J Med Chem. 2017. PMID: 28714680 No abstract available.
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia.
Tron AE, Belmonte MA, Adam A, Aquila BM, Boise LH, Chiarparin E, Cidado J, Embrey KJ, Gangl E, Gibbons FD, Gregory GP, Hargreaves D, Hendricks JA, Johannes JW, Johnstone RW, Kazmirski SL, Kettle JG, Lamb ML, Matulis SM, Nooka AK, Packer MJ, Peng B, Rawlins PB, Robbins DW, Schuller AG, Su N, Yang W, Ye Q, Zheng X, Secrist JP, Clark EA, Wilson DM, Fawell SE, Hird AW. Tron AE, et al. Nat Commun. 2018 Dec 17;9(1):5341. doi: 10.1038/s41467-018-07551-w. Nat Commun. 2018. PMID: 30559424 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
AZD4320, A Dual Inhibitor of Bcl-2 and Bcl-xL, Induces Tumor Regression in Hematologic Cancer Models without Dose-limiting Thrombocytopenia.
Balachander SB, Criscione SW, Byth KF, Cidado J, Adam A, Lewis P, Macintyre T, Wen S, Lawson D, Burke K, Lubinski T, Tyner JW, Kurtz SE, McWeeney SK, Varnes J, Diebold RB, Gero T, Ioannidis S, Hennessy EJ, McCoull W, Saeh JC, Tabatabai A, Tavana O, Su N, Schuller A, Garnett MJ, Jaaks P, Coker EA, Gregory GP, Newbold A, Johnstone RW, Gangl E, Wild M, Zinda M, Secrist JP, Davies BR, Fawell SE, Gibbons FD. Balachander SB, et al. Clin Cancer Res. 2020 Dec 15;26(24):6535-6549. doi: 10.1158/1078-0432.CCR-20-0863. Epub 2020 Sep 28. Clin Cancer Res. 2020. PMID: 32988967
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. Among authors: gangl et. 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.
37 results