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3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
Hewings DS, Wang M, Philpott M, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Vuppusetty C, Marsden B, Knapp S, Conway SJ, Heightman TD. Hewings DS, et al. Among authors: conway sj. J Med Chem. 2011 Oct 13;54(19):6761-70. doi: 10.1021/jm200640v. Epub 2011 Sep 6. J Med Chem. 2011. PMID: 21851057 Free PMC article.
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
Hewings DS, Fedorov O, Filippakopoulos P, Martin S, Picaud S, Tumber A, Wells C, Olcina MM, Freeman K, Gill A, Ritchie AJ, Sheppard DW, Russell AJ, Hammond EM, Knapp S, Brennan PE, Conway SJ. Hewings DS, et al. Among authors: conway sj. J Med Chem. 2013 Apr 25;56(8):3217-27. doi: 10.1021/jm301588r. Epub 2013 Apr 5. J Med Chem. 2013. PMID: 23517011 Free PMC article.
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
Jennings LE, Schiedel M, Hewings DS, Picaud S, Laurin CMC, Bruno PA, Bluck JP, Scorah AR, See L, Reynolds JK, Moroglu M, Mistry IN, Hicks A, Guzanov P, Clayton J, Evans CNG, Stazi G, Biggin PC, Mapp AK, Hammond EM, Humphreys PG, Filippakopoulos P, Conway SJ. Jennings LE, et al. Among authors: conway sj. Bioorg Med Chem. 2018 Jul 15;26(11):2937-2957. doi: 10.1016/j.bmc.2018.05.003. Epub 2018 May 15. Bioorg Med Chem. 2018. PMID: 29776834 Free article.
Bifunctional Molecules beyond PROTACs.
Conway SJ. Conway SJ. J Med Chem. 2020 Mar 26;63(6):2802-2806. doi: 10.1021/acs.jmedchem.0c00293. Epub 2020 Mar 11. J Med Chem. 2020. PMID: 32157887
333 results