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Items: 22

1.

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition.

Wyllie S, Brand S, Thomas M, De Rycker M, Chung CW, Pena I, Bingham RP, Bueren-Calabuig JA, Cantizani J, Cebrian D, Craggs PD, Ferguson L, Goswami P, Hobrath J, Howe J, Jeacock L, Ko EJ, Korczynska J, MacLean L, Manthri S, Martinez MS, Mata-Cantero L, Moniz S, Nühs A, Osuna-Cabello M, Pinto E, Riley J, Robinson S, Rowland P, Simeons FRC, Shishikura Y, Spinks D, Stojanovski L, Thomas J, Thompson S, Viayna Gaza E, Wall RJ, Zuccotto F, Horn D, Ferguson MAJ, Fairlamb AH, Fiandor JM, Martin J, Gray DW, Miles TJ, Gilbert IH, Read KD, Marco M, Wyatt PG.

Proc Natl Acad Sci U S A. 2019 May 7;116(19):9318-9323. doi: 10.1073/pnas.1820175116. Epub 2019 Apr 8.

2.

Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis.

Thomas MG, De Rycker M, Ajakane M, Albrecht S, Álvarez-Pedraglio AI, Boesche M, Brand S, Campbell L, Cantizani-Perez J, Cleghorn LAT, Copley RCB, Crouch SD, Daugan A, Drewes G, Ferrer S, Ghidelli-Disse S, Gonzalez S, Gresham SL, Hill AP, Hindley SJ, Lowe RM, MacKenzie CJ, MacLean L, Manthri S, Martin F, Miguel-Siles J, Nguyen VL, Norval S, Osuna-Cabello M, Woodland A, Patterson S, Pena I, Quesada-Campos MT, Reid IH, Revill C, Riley J, Ruiz-Gomez JR, Shishikura Y, Simeons FRC, Smith A, Smith VC, Spinks D, Stojanovski L, Thomas J, Thompson S, Underwood T, Gray DW, Fiandor JM, Gilbert IH, Wyatt PG, Read KD, Miles TJ.

J Med Chem. 2019 Feb 14;62(3):1180-1202. doi: 10.1021/acs.jmedchem.8b01218. Epub 2018 Dec 20.

3.

2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas' disease.

Thomas MG, De Rycker M, Cotillo Torrejon I, Thomas J, Riley J, Spinks D, Read KD, Miles TJ, Gilbert IH, Wyatt PG.

Bioorg Med Chem Lett. 2018 Oct 1;28(18):3025-3030. doi: 10.1016/j.bmcl.2018.08.005. Epub 2018 Aug 3.

PMID:
30104093
4.

Screening a protein kinase inhibitor library against Plasmodium falciparum.

Hallyburton I, Grimaldi R, Woodland A, Baragaña B, Luksch T, Spinks D, James D, Leroy D, Waterson D, Fairlamb AH, Wyatt PG, Gilbert IH, Frearson JA.

Malar J. 2017 Nov 7;16(1):446. doi: 10.1186/s12936-017-2085-4.

5.

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.

Brand S, Ko EJ, Viayna E, Thompson S, Spinks D, Thomas M, Sandberg L, Francisco AF, Jayawardhana S, Smith VC, Jansen C, De Rycker M, Thomas J, MacLean L, Osuna-Cabello M, Riley J, Scullion P, Stojanovski L, Simeons FRC, Epemolu O, Shishikura Y, Crouch SD, Bakshi TS, Nixon CJ, Reid IH, Hill AP, Underwood TZ, Hindley SJ, Robinson SA, Kelly JM, Fiandor JM, Wyatt PG, Marco M, Miles TJ, Read KD, Gilbert IH.

J Med Chem. 2017 Sep 14;60(17):7284-7299. doi: 10.1021/acs.jmedchem.7b00463. Epub 2017 Aug 27.

6.

Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode.

Spinks D, Smith V, Thompson S, Robinson DA, Luksch T, Smith A, Torrie LS, McElroy S, Stojanovski L, Norval S, Collie IT, Hallyburton I, Rao B, Brand S, Brenk R, Frearson JA, Read KD, Wyatt PG, Gilbert IH.

ChemMedChem. 2015 Nov;10(11):1821-36. doi: 10.1002/cmdc.201500301. Epub 2015 Sep 23.

7.

Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors.

Spinks D, Torrie LS, Thompson S, Harrison JR, Frearson JA, Read KD, Fairlamb AH, Wyatt PG, Gilbert IH.

ChemMedChem. 2012 Jan 2;7(1):95-106. doi: 10.1002/cmdc.201100420. Epub 2011 Dec 8.

8.

Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors.

Brand S, Cleghorn LA, McElroy SP, Robinson DA, Smith VC, Hallyburton I, Harrison JR, Norcross NR, Spinks D, Bayliss T, Norval S, Stojanovski L, Torrie LS, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Read KD, Wyatt PG, Gilbert IH.

J Med Chem. 2012 Jan 12;55(1):140-52. doi: 10.1021/jm201091t. Epub 2011 Dec 7.

9.

Optimisation of the anti-Trypanosoma brucei activity of the opioid agonist U50488.

Smith VC, Cleghorn LA, Woodland A, Spinks D, Hallyburton I, Collie IT, Mok NY, Norval S, Brenk R, Fairlamb AH, Frearson JA, Read KD, Gilbert IH, Wyatt PG.

ChemMedChem. 2011 Oct 4;6(10):1832-40. doi: 10.1002/cmdc.201100278. Epub 2011 Aug 10.

10.

Design, synthesis and biological evaluation of novel inhibitors of Trypanosoma brucei pteridine reductase 1.

Spinks D, Ong HB, Mpamhanga CP, Shanks EJ, Robinson DA, Collie IT, Read KD, Frearson JA, Wyatt PG, Brenk R, Fairlamb AH, Gilbert IH.

ChemMedChem. 2011 Feb 7;6(2):302-8. doi: 10.1002/cmdc.201000450. Epub 2010 Dec 29.

11.

The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.

Reid M, Carlyle I, Caulfield WL, Clarkson TR, Cusick F, Epemolu O, Gilfillan R, Goodwin R, Jaap D, O'Donnell EC, Presland J, Rankovic Z, Spinks D, Spinks G, Thomson AM, Thomson F, Strain J, Wishart G.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3713-6. doi: 10.1016/j.bmcl.2010.04.085. Epub 2010 Apr 24.

PMID:
20471831
12.

Investigation of trypanothione reductase as a drug target in Trypanosoma brucei.

Spinks D, Shanks EJ, Cleghorn LA, McElroy S, Jones D, James D, Fairlamb AH, Frearson JA, Wyatt PG, Gilbert IH.

ChemMedChem. 2009 Dec;4(12):2060-9. doi: 10.1002/cmdc.200900262.

13.

Chemical validation of trypanothione synthetase: a potential drug target for human trypanosomiasis.

Torrie LS, Wyllie S, Spinks D, Oza SL, Thompson S, Harrison JR, Gilbert IH, Wyatt PG, Fairlamb AH, Frearson JA.

J Biol Chem. 2009 Dec 25;284(52):36137-45. doi: 10.1074/jbc.M109.045336. Epub 2009 Oct 14.

14.

Dissecting the essentiality of the bifunctional trypanothione synthetase-amidase in Trypanosoma brucei using chemical and genetic methods.

Wyllie S, Oza SL, Patterson S, Spinks D, Thompson S, Fairlamb AH.

Mol Microbiol. 2009 Nov;74(3):529-40. doi: 10.1111/j.1365-2958.2009.06761.x. Epub 2009 Jun 24.

15.

One scaffold, three binding modes: novel and selective pteridine reductase 1 inhibitors derived from fragment hits discovered by virtual screening.

Mpamhanga CP, Spinks D, Tulloch LB, Shanks EJ, Robinson DA, Collie IT, Fairlamb AH, Wyatt PG, Frearson JA, Hunter WN, Gilbert IH, Brenk R.

J Med Chem. 2009 Jul 23;52(14):4454-65. doi: 10.1021/jm900414x.

16.

2-Aryl-3,3,3-trifluoro-2-hydroxypropionic acids: a new class of protein tyrosine phosphatase 1B inhibitors.

Adams DR, Abraham A, Asano J, Breslin C, Dick CA, Ixkes U, Johnston BF, Johnston D, Kewnay J, Mackay SP, MacKenzie SJ, McFarlane M, Mitchell L, Spinks D, Takano Y.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6579-83. Epub 2007 Sep 25.

PMID:
17931864
17.

Cyclic nucleotide signalling: a molecular approach to drug discovery for Alzheimer's disease.

McPhee I, Gibson LC, Kewney J, Darroch C, Stevens PA, Spinks D, Cooreman A, MacKenzie SJ.

Biochem Soc Trans. 2005 Dec;33(Pt 6):1330-2. Review.

PMID:
16246111
18.

Serotonin reuptake inhibition: an update on current research strategies.

Spinks D, Spinks G.

Curr Med Chem. 2002 Apr;9(8):799-810. Review.

PMID:
11966445
19.

4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.

Fletcher SR, Burkamp F, Blurton P, Cheng SK, Clarkson R, O'Connor D, Spinks D, Tudge M, van Niel MB, Patel S, Chapman K, Marwood R, Shepheard S, Bentley G, Cook GP, Bristow LJ, Castro JL, Hutson PH, MacLeod AM.

J Med Chem. 2002 Jan 17;45(2):492-503.

PMID:
11784153
20.

Measurement of the speed of sound in ethanol/water mixtures.

Martin K, Spinks D.

Ultrasound Med Biol. 2001 Feb;27(2):289-91.

PMID:
11316539
21.

Biaryl acids: novel non-nucleoside inhibitors of HIV reverse transcriptase types 1 and 2.

Milton J, Slater MJ, Bird AJ, Spinks D, Scott G, Price CE, Downing S, Green DV, Madar S, Bethell R, Stammers DK.

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2623-8. Review.

PMID:
9873592
22.

Campylobacter gastroenteritis in Arkansas.

May J, Spinks D, Estes K, McAtee R.

J Ark Med Soc. 1982 Nov;79(6):191-3. No abstract available.

PMID:
6217185

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