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Items: 14

1.

Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase.

Read J, Collie IT, Nguyen-McCarty M, Lucaj C, Robinson J, Conway L, Mukherjee J, McCall E, Donohoe G, Flavell E, Peciak K, Warwicker J, Dix C, Van den Hoven BG, Madin A, Brown DG, Moss S, Haggarty SJ, Brandon NJ, Bürli RW.

Bioorg Med Chem Lett. 2019 Aug 1;29(15):1962-1967. doi: 10.1016/j.bmcl.2019.05.032. Epub 2019 May 18.

PMID:
31153805
2.

Acid-Mediated Ring Expansion of 2,2-Disubstituted Azetidine Carbamates to 6,6-Disubstituted 1,3-Oxazinan-2-ones.

Boddy AJ, Cordier CJ, Goldberg K, Madin A, Spivey AC, Bull JA.

Org Lett. 2019 Mar 15;21(6):1818-1822. doi: 10.1021/acs.orglett.9b00407. Epub 2019 Mar 4.

PMID:
30829041
3.

Synthesis of Structurally Diverse N-Substituted Quaternary-Carbon-Containing Small Molecules from α,α-Disubstituted Propargyl Amino Esters.

Mateu N, Kidd SL, Kalash L, Sore HF, Madin A, Bender A, Spring DR.

Chemistry. 2018 Sep 12;24(51):13681-13687. doi: 10.1002/chem.201803143. Epub 2018 Aug 13.

4.

Partially Saturated Bicyclic Heteroaromatics as an sp(3) -Enriched Fragment Collection.

Twigg DG, Kondo N, Mitchell SL, Galloway WR, Sore HF, Madin A, Spring DR.

Angew Chem Int Ed Engl. 2016 Sep 26;55(40):12479-83. doi: 10.1002/anie.201606496. Epub 2016 Sep 6.

5.

Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition.

Ellard JM, Madin A, Philps O, Hopkin M, Henderson S, Birch L, O'Connor D, Arai T, Takase K, Morgan L, Reynolds D, Talma S, Howley E, Powney B, Payne AH, Hall A, Gartlon JE, Dawson LA, Castro L, Atkinson PJ.

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5792-6. doi: 10.1016/j.bmcl.2015.10.050. Epub 2015 Oct 17.

PMID:
26531152
6.

Potent, selective inhibitors of fibroblast growth factor receptor define fibroblast growth factor dependence in preclinical cancer models.

Squires M, Ward G, Saxty G, Berdini V, Cleasby A, King P, Angibaud P, Perera T, Fazal L, Ross D, Jones CG, Madin A, Benning RK, Vickerstaffe E, O'Brien A, Frederickson M, Reader M, Hamlett C, Batey MA, Rich S, Carr M, Miller D, Feltell R, Thiru A, Bethell S, Devine LA, Graham BL, Pike A, Cosme J, Lewis EJ, Freyne E, Lyons J, Irving J, Murray C, Newell DR, Thompson NT.

Mol Cancer Ther. 2011 Sep;10(9):1542-52. doi: 10.1158/1535-7163.MCT-11-0426. Epub 2011 Jul 15.

7.

Novel orally bioavailable gamma-secretase inhibitors with excellent in vivo activity.

Keown LE, Collins I, Cooper LC, Harrison T, Madin A, Mistry J, Reilly M, Shaimi M, Welch CJ, Clarke EE, Lewis HD, Wrigley JD, Best JD, Murray F, Shearman MS.

J Med Chem. 2009 Jun 11;52(11):3441-4. doi: 10.1021/jm900056p.

PMID:
19432431
8.

Sulfonamide derivatives of bridgehead substituted bicyclo[4.2.1]nonanes as gamma-secretase inhibitors.

Sparey T, Clarke E, Hannam J, Harrison T, Madin A, Shearman M, Sohal B.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):375-9. Epub 2007 Oct 22.

PMID:
18061448
9.

Apoptosis in T cell acute lymphoblastic leukemia cells after cell cycle arrest induced by pharmacological inhibition of notch signaling.

Lewis HD, Leveridge M, Strack PR, Haldon CD, O'neil J, Kim H, Madin A, Hannam JC, Look AT, Kohl N, Draetta G, Harrison T, Kerby JA, Shearman MS, Beher D.

Chem Biol. 2007 Feb;14(2):209-19.

10.
11.

Aza-cope rearrangement-mannich cyclizations for the formation of complex tricyclic amines: stereocontrolled total synthesis of (+/-)-gelsemine.

Earley WG, Jacobsen JE, Madin A, Meier GP, O'Donnell CJ, Oh T, Old DW, Overman LE, Sharp MJ.

J Am Chem Soc. 2005 Dec 28;127(51):18046-53.

12.

7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.

Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ.

J Med Chem. 2005 Nov 17;48(23):7089-92.

PMID:
16279764
13.

Cyclic sulfamide gamma-secretase inhibitors.

Sparey T, Beher D, Best J, Biba M, Castro JL, Clarke E, Hannam J, Harrison T, Lewis H, Madin A, Shearman M, Sohal B, Tsou N, Welch C, Wrigley J.

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4212-6.

PMID:
16054361
14.

Total Synthesis of (+/-)-Gelsemine.

Madin A, O'Donnell CJ, Oh T, Old DW, Overman LE, Sharp MJ.

Angew Chem Int Ed Engl. 1999 Oct 4;38(19):2934-2936.

PMID:
10540398

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