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Items: 13

1.

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.

Cancer Res. 2016 Jun 1;76(11):3307-18. doi: 10.1158/0008-5472.CAN-15-2357. Epub 2016 Mar 28.

2.

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.

J Med Chem. 2016 Apr 14;59(7):3576. doi: 10.1021/acs.jmedchem.6b00364. Epub 2016 Mar 22. No abstract available.

PMID:
27003331
3.

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.

J Med Chem. 2015 Oct 22;58(20):8128-40. doi: 10.1021/acs.jmedchem.5b00984. Epub 2015 Oct 7.

PMID:
26407012
4.

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.

J Med Chem. 2015 Apr 23;58(8):3522-33. doi: 10.1021/acs.jmedchem.5b00066. Epub 2015 Apr 1. Erratum in: J Med Chem. 2016 Apr 14;59(7):3576.

PMID:
25790336
5.

Efficacious inhaled PDE4 inhibitors with low emetic potential and long duration of action for the treatment of COPD.

De Savi C, Cox RJ, Warner DJ, Cook AR, Dickinson MR, McDonough A, Morrill LC, Parker B, Andrews G, Young SS, Gilmour PS, Riley R, Dearman MS.

J Med Chem. 2014 Jun 12;57(11):4661-76. doi: 10.1021/jm5001216. Epub 2014 May 30.

PMID:
24785301
6.

Hydantoin based inhibitors of MMP13--discovery of AZD6605.

De Savi C, Waterson D, Pape A, Lamont S, Hadley E, Mills M, Page KM, Bowyer J, Maciewicz RA.

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4705-12. doi: 10.1016/j.bmcl.2013.05.089. Epub 2013 Jun 10.

PMID:
23810497
7.

Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2.

De Savi C, Morley AD, Nash I, Karoutchi G, Page K, Ting A, Gerhardt S.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):271-7. doi: 10.1016/j.bmcl.2011.11.034. Epub 2011 Nov 16.

PMID:
22153941
8.

Selective non zinc binding inhibitors of MMP13.

De Savi C, Morley AD, Ting A, Nash I, Karabelas K, Wood CM, James M, Norris SJ, Karoutchi G, Rankine N, Hamlin G, Macfaul PA, Ryan D, Baker SV, Hargreaves D, Gerhardt S.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4215-9. doi: 10.1016/j.bmcl.2011.05.075. Epub 2011 May 27.

PMID:
21669521
9.

Orally active achiral N-hydroxyformamide inhibitors of ADAM-TS4 (aggrecanase-1) and ADAM-TS5 (aggrecanase-2) for the treatment of osteoarthritis.

De Savi C, Pape A, Sawyer Y, Milne D, Davies C, Cumming JG, Ting A, Lamont S, Smith PD, Tart J, Page K, Moore P.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3301-6. doi: 10.1016/j.bmcl.2011.04.028. Epub 2011 Apr 13.

PMID:
21536437
10.

The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.

De Savi C, Pape A, Cumming JG, Ting A, Smith PD, Burrows JN, Mills M, Davies C, Lamont S, Milne D, Cook C, Moore P, Sawyer Y, Gerhardt S.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1376-81. doi: 10.1016/j.bmcl.2011.01.036. Epub 2011 Jan 18.

PMID:
21300546
11.

Construction of perhydro indol-2-ones by a methoxide catalyzed deacetylation-Michael-aldol cascade.

Ward JW, Dodd K, Rigby CL, De Savi C, Dixon DJ.

Chem Commun (Camb). 2010 Mar 14;46(10):1691-3. doi: 10.1039/b924637a. Epub 2010 Jan 13.

PMID:
20177618
12.

Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.

Mortlock AA, Foote KM, Heron NM, Jung FH, Pasquet G, Lohmann JJ, Warin N, Renaud F, De Savi C, Roberts NJ, Johnson T, Dousson CB, Hill GB, Perkins D, Hatter G, Wilkinson RW, Wedge SR, Heaton SP, Odedra R, Keen NJ, Crafter C, Brown E, Thompson K, Brightwell S, Khatri L, Brady MC, Kearney S, McKillop D, Rhead S, Parry T, Green S.

J Med Chem. 2007 May 3;50(9):2213-24. Epub 2007 Mar 21.

PMID:
17373783
13.

Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.

Jung FH, Pasquet G, Lambert-van der Brempt C, Lohmann JJ, Warin N, Renaud F, Germain H, De Savi C, Roberts N, Johnson T, Dousson C, Hill GB, Mortlock AA, Heron N, Wilkinson RW, Wedge SR, Heaton SP, Odedra R, Keen NJ, Green S, Brown E, Thompson K, Brightwell S.

J Med Chem. 2006 Feb 9;49(3):955-70.

PMID:
16451062

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