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Page 1
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).
Bradbury RH, Callis R, Carr GR, Chen H, Clark E, Feron L, Glossop S, Graham MA, Hattersley M, Jones C, Lamont SG, Ouvry G, Patel A, Patel J, Rabow AA, Roberts CA, Stokes S, Stratton N, Walker GE, Ward L, Whalley D, Whittaker D, Wrigley G, Waring MJ. Bradbury RH, et al. Among authors: callis r. J Med Chem. 2016 Sep 8;59(17):7801-17. doi: 10.1021/acs.jmedchem.6b00070. Epub 2016 Aug 24. J Med Chem. 2016. PMID: 27528113
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: callis rj. 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
Potent and selective bivalent inhibitors of BET bromodomains.
Waring MJ, Chen H, Rabow AA, Walker G, Bobby R, Boiko S, Bradbury RH, Callis R, Clark E, Dale I, Daniels DL, Dulak A, Flavell L, Holdgate G, Jowitt TA, Kikhney A, McAlister M, Méndez J, Ogg D, Patel J, Petteruti P, Robb GR, Robers MB, Saif S, Stratton N, Svergun DI, Wang W, Whittaker D, Wilson DM, Yao Y. Waring MJ, et al. Among authors: callis r. Nat Chem Biol. 2016 Dec;12(12):1097-1104. doi: 10.1038/nchembio.2210. Epub 2016 Oct 24. Nat Chem Biol. 2016. PMID: 27775716
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. Among authors: callis rj. 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
Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.
Degorce SL, Bailey A, Callis R, De Savi C, Ducray R, Lamont G, MacFaul P, Maudet M, Martin S, Morgentin R, Norman RA, Peru A, Pink JH, Plé PA, Roberts B, Scott JS. Degorce SL, et al. Among authors: callis r. J Med Chem. 2015 Apr 23;58(8):3522-33. doi: 10.1021/acs.jmedchem.5b00066. Epub 2015 Apr 1. J Med Chem. 2015. PMID: 25790336
AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer.
Hickinson DM, Klinowska T, Speake G, Vincent J, Trigwell C, Anderton J, Beck S, Marshall G, Davenport S, Callis R, Mills E, Grosios K, Smith P, Barlaam B, Wilkinson RW, Ogilvie D. Hickinson DM, et al. Among authors: callis r. Clin Cancer Res. 2010 Feb 15;16(4):1159-69. doi: 10.1158/1078-0432.CCR-09-2353. Epub 2010 Feb 9. Clin Cancer Res. 2010. PMID: 20145185
Correction to Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.
Degorce SL, Bailey A, Callis R, De Savi C, Ducray R, Lamont G, MacFaul P, Maudet M, Martin S, Morgentin R, Norman RA, Peru A, Pink JH, Plé PA, Roberts B, Scott JS. Degorce SL, et al. Among authors: callis r. J Med Chem. 2016 Apr 14;59(7):3576. doi: 10.1021/acs.jmedchem.6b00364. Epub 2016 Mar 22. J Med Chem. 2016. PMID: 27003331 No abstract available.
18 results