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1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ, Le Gall A, Michon AM, Mitchell DJ, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ. Demont EH, et al. Among authors: bamborough p. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5. doi: 10.1021/ml5002932. eCollection 2014 Nov 13. ACS Med Chem Lett. 2014. PMID: 25408830 Free PMC article.
Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.
Preston A, Atkinson S, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Gray JRJ, Jones EJ, Lindon M, Michon AM, Mitchell DJ, Prinjha RK, Rianjongdee F, Rioja I, Seal J, Taylor S, Wall I, Watson RJ, Woolven J, Demont EH. Preston A, et al. Among authors: bamborough p. J Med Chem. 2020 Sep 10;63(17):9070-9092. doi: 10.1021/acs.jmedchem.0c00605. Epub 2020 Aug 20. J Med Chem. 2020. PMID: 32691591
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Wellaway CR, Bamborough P, Bernard SG, Chung CW, Craggs PD, Cutler L, Demont EH, Evans JP, Gordon L, Karamshi B, Lewis AJ, Lindon MJ, Mitchell DJ, Rioja I, Soden PE, Taylor S, Watson RJ, Willis R, Woolven JM, Wyspiańska BS, Kerr WJ, Prinjha RK. Wellaway CR, et al. Among authors: bamborough p. J Med Chem. 2020 Sep 10;63(17):9020-9044. doi: 10.1021/acs.jmedchem.0c00566. Epub 2020 Aug 3. J Med Chem. 2020. PMID: 32787145 Free article.
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
Preston A, Atkinson SJ, Bamborough P, Chung CW, Gordon LJ, Grandi P, Gray JRJ, Harrison LA, Lewis AJ, Lugo D, Messenger C, Michon AM, Mitchell DJ, Prinjha RK, Rioja I, Seal J, Taylor S, Thesmar P, Wall ID, Watson RJ, Woolven JM, Demont EH. Preston A, et al. Among authors: bamborough p. ACS Med Chem Lett. 2020 Jul 6;11(8):1581-1587. doi: 10.1021/acsmedchemlett.0c00247. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 32832027 Free PMC article.
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Aylott HE, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Gordon L, Grandi P, Gray JRJ, Harrison LA, Hayhow TG, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Seal JT, Wall ID, Watson RJ, Woolven JM, Demont EH. Aylott HE, et al. Among authors: bamborough p. J Med Chem. 2021 Mar 25;64(6):3249-3281. doi: 10.1021/acs.jmedchem.0c02156. Epub 2021 Mar 4. J Med Chem. 2021. PMID: 33662213
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Seal JT, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Foley J, Gordon L, Grandi P, Gray JRJ, Harrison LA, Kruger RG, Matteo JJ, McCabe MT, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Taylor S, Wall ID, Watson RJ, Woolven JM, Wyce A, Zhang XP, Demont EH. Seal JT, et al. Among authors: bamborough p. J Med Chem. 2021 Aug 12;64(15):10772-10805. doi: 10.1021/acs.jmedchem.1c00365. Epub 2021 Jul 13. J Med Chem. 2021. PMID: 34255512
Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.
Clegg MA, Theodoulou NH, Bamborough P, Chung CW, Craggs PD, Demont EH, Gordon LJ, Liwicki GM, Phillipou A, Tomkinson NCO, Prinjha RK, Humphreys PG. Clegg MA, et al. Among authors: bamborough p. ACS Med Chem Lett. 2021 Aug 3;12(8):1308-1317. doi: 10.1021/acsmedchemlett.1c00294. eCollection 2021 Aug 12. ACS Med Chem Lett. 2021. PMID: 34413961 Free PMC article.
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Humphreys PG, Atkinson SJ, Bamborough P, Bit RA, Chung CW, Craggs PD, Cutler L, Davis R, Ferrie A, Gong G, Gordon LJ, Gray M, Harrison LA, Hayhow TG, Haynes A, Henley N, Hirst DJ, Holyer ID, Lindon MJ, Lovatt C, Lugo D, McCleary S, Molnar J, Osmani Q, Patten C, Preston A, Rioja I, Seal JT, Smithers N, Sun F, Tang D, Taylor S, Theodoulou NH, Thomas C, Watson RJ, Wellaway CR, Zhu L, Tomkinson NCO, Prinjha RK. Humphreys PG, et al. Among authors: bamborough p. J Med Chem. 2022 Feb 10;65(3):2262-2287. doi: 10.1021/acs.jmedchem.1c01747. Epub 2022 Jan 7. J Med Chem. 2022. PMID: 34995458 Free article.
82 results