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Items: 39

1.

New approaches for the treatment of Alzheimer's disease.

Fish PV, Steadman D, Bayle ED, Whiting P.

Bioorg Med Chem Lett. 2019 Jan 15;29(2):125-133. doi: 10.1016/j.bmcl.2018.11.034. Epub 2018 Nov 19. Review.

PMID:
30501965
2.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. No abstract available.

3.

Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains.

Le Manach C, Paquet T, Wicht K, Nchinda AT, Brunschwig C, Njoroge M, Gibhard L, Taylor D, Lawrence N, Wittlin S, Eyermann CJ, Basarab GS, Duffy J, Fish PV, Street LJ, Chibale K.

J Med Chem. 2018 Oct 25;61(20):9371-9385. doi: 10.1021/acs.jmedchem.8b01333. Epub 2018 Oct 16.

PMID:
30256636
4.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Erratum in: Antimicrob Agents Chemother. 2018 Oct 24;62(11):.

PMID:
29941635
5.

Regioselective and enantiospecific synthesis of the HSP co-inducer arimoclomol from chiral glycidyl derivatives.

Atkinson BN, Woodward HL, Sipthorp J, Fish PV.

Org Biomol Chem. 2017 Nov 29;15(46):9794-9799. doi: 10.1039/c7ob02578e.

PMID:
29159344
6.

Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation.

Meier JC, Tallant C, Fedorov O, Witwicka H, Hwang SY, van Stiphout RG, Lambert JP, Rogers C, Yapp C, Gerstenberger BS, Fedele V, Savitsky P, Heidenreich D, Daniels DL, Owen DR, Fish PV, Igoe NM, Bayle ED, Haendler B, Oppermann UCT, Buffa F, Brennan PE, Müller S, Gingras AC, Odgren PR, Birnbaum MJ, Knapp S.

ACS Chem Biol. 2017 Oct 20;12(10):2619-2630. doi: 10.1021/acschembio.7b00481. Epub 2017 Sep 12.

7.

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.

Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Müller S, Knapp S, Fish PV.

J Med Chem. 2017 Aug 24;60(16):6998-7011. doi: 10.1021/acs.jmedchem.7b00611. Epub 2017 Aug 10.

PMID:
28714688
8.

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.

Igoe N, Bayle ED, Fedorov O, Tallant C, Savitsky P, Rogers C, Owen DR, Deb G, Somervaille TC, Andrews DM, Jones N, Cheasty A, Ryder H, Brennan PE, Müller S, Knapp S, Fish PV.

J Med Chem. 2017 Jan 26;60(2):668-680. doi: 10.1021/acs.jmedchem.6b01583. Epub 2017 Jan 9.

PMID:
28068087
9.

New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.

Spurr SS, Bayle ED, Yu W, Li F, Tempel W, Vedadi M, Schapira M, Fish PV.

Bioorg Med Chem Lett. 2016 Sep 15;26(18):4518-4522. doi: 10.1016/j.bmcl.2016.07.041. Epub 2016 Jul 21.

PMID:
27485386
10.

Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.

Rouquet G, Moore DE, Spain M, Allwood DM, Battilocchio C, Blakemore DC, Fish PV, Jenkinson S, Jessiman AS, Ley SV, McMurray G, Storer RI.

ACS Med Chem Lett. 2015 Jan 20;6(3):329-33. doi: 10.1021/ml500507v. eCollection 2015 Mar 12.

11.

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.

Barsyte-Lovejoy D, Li F, Oudhoff MJ, Tatlock JH, Dong A, Zeng H, Wu H, Freeman SA, Schapira M, Senisterra GA, Kuznetsova E, Marcellus R, Allali-Hassani A, Kennedy S, Lambert JP, Couzens AL, Aman A, Gingras AC, Al-Awar R, Fish PV, Gerstenberger BS, Roberts L, Benn CL, Grimley RL, Braam MJ, Rossi FM, Sudol M, Brown PJ, Bunnage ME, Owen DR, Zaph C, Vedadi M, Arrowsmith CH.

Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8. doi: 10.1073/pnas.1407358111. Epub 2014 Aug 18.

12.

Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors.

Storer RI, Brennan PE, Brown AD, Bungay PJ, Conlon KM, Corbett MS, DePianta RP, Fish PV, Heifetz A, Ho DK, Jessiman AS, McMurray G, de Oliveira CA, Roberts LR, Root JA, Shanmugasundaram V, Shapiro MJ, Skerten M, Westbrook D, Wheeler S, Whitlock GA, Wright J.

J Med Chem. 2014 Jun 26;57(12):5258-69. doi: 10.1021/jm5003292. Epub 2014 Jun 17.

PMID:
24878222
13.

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.

Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Müller S, Schwaller J, Stankovic T, Knapp S.

Cancer Res. 2013 Jun 1;73(11):3336-46. doi: 10.1158/0008-5472.CAN-12-3292. Epub 2013 Apr 10.

14.

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.

Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, Primiano MJ, Ralph MJ, Sciammetta N, Trzupek JD.

J Med Chem. 2012 Nov 26;55(22):9831-7. doi: 10.1021/jm3010515. Epub 2012 Nov 8.

15.

Epigenetic protein families: a new frontier for drug discovery.

Arrowsmith CH, Bountra C, Fish PV, Lee K, Schapira M.

Nat Rev Drug Discov. 2012 Apr 13;11(5):384-400. doi: 10.1038/nrd3674. Review.

PMID:
22498752
16.

Bridging solubility between drug discovery and development.

Di L, Fish PV, Mano T.

Drug Discov Today. 2012 May;17(9-10):486-95. doi: 10.1016/j.drudis.2011.11.007. Epub 2011 Nov 26. Review.

PMID:
22138563
17.

Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.

Andrews MD, Fish PV, Blagg J, Brabham TK, Brennan PE, Bridgeland A, Brown AD, Bungay PJ, Conlon KM, Edmunds NJ, af Forselles K, Gibbons CP, Green MP, Hanton G, Holbrook M, Jessiman AS, McIntosh K, McMurray G, Nichols CL, Root JA, Storer RI, Sutton MR, Ward RV, Westbrook D, Whitlock GA.

Bioorg Med Chem Lett. 2011 May 1;21(9):2715-20. doi: 10.1016/j.bmcl.2010.11.120. Epub 2010 Dec 4.

PMID:
21195614
18.

Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.

Fray MJ, Fish PV, Allan GA, Bish G, Clarke N, Eccles R, Harrison AC, Le Net JL, Phillips SC, Regan N, Sobry C, Stobie A, Wakenhut F, Westbrook D, Westbrook SL, Whitlock GA.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92. doi: 10.1016/j.bmcl.2010.04.052. Epub 2010 Apr 18.

PMID:
20471260
19.

The Scar-in-a-Jar: studying potential antifibrotic compounds from the epigenetic to extracellular level in a single well.

Chen CZ, Peng YX, Wang ZB, Fish PV, Kaar JL, Koepsel RR, Russell AJ, Lareu RR, Raghunath M.

Br J Pharmacol. 2009 Nov;158(5):1196-209. doi: 10.1111/j.1476-5381.2009.00387.x. Epub 2009 Sep 28.

20.

N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.

Wakenhut F, Allan GA, Fish PV, Fray MJ, Harrison AC, McCoy R, Phillips SC, Ryckmans T, Stobie A, Westbrook D, Westbrook SL, Whitlock GA.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5078-81. doi: 10.1016/j.bmcl.2009.07.049. Epub 2009 Jul 31. Erratum in: Bioorg Med Chem Lett. 2010 Jan 15;20(2):772. Ryckmans, Thomas [added].

PMID:
19647430
21.

Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.

Fish PV, Wakenhut F, Ryckmans T, Stobie A.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83. doi: 10.1016/j.bmcl.2009.06.096. Epub 2009 Jul 2.

PMID:
19616432
22.

6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists.

Roberts LR, Fish PV, Ian Storer R, Whitlock GA.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3113-7. doi: 10.1016/j.bmcl.2009.03.166. Epub 2009 Apr 18.

PMID:
19414260
23.

4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships.

Fish PV, Andrews MD, Jonathan Fray M, Stobie A, Wakenhut F, Whitlock GA.

Bioorg Med Chem Lett. 2009 May 15;19(10):2829-34. doi: 10.1016/j.bmcl.2009.03.090. Epub 2009 Mar 26.

PMID:
19359175
24.

7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization.

Fish PV, Brown AD, Evrard E, Roberts LR.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):1871-5. doi: 10.1016/j.bmcl.2009.02.071. Epub 2009 Feb 21.

PMID:
19269173
25.

Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.

Bailey S, Fish PV, Billotte S, Bordner J, Greiling D, James K, McElroy A, Mills JE, Reed C, Webster R.

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6562-7. doi: 10.1016/j.bmcl.2008.10.036. Epub 2008 Oct 11.

PMID:
18945617
26.

N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors.

Wakenhut F, Fish PV, Fray MJ, Gurrell I, Mills JE, Stobie A, Whitlock GA.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4308-11. doi: 10.1016/j.bmcl.2008.06.078. Epub 2008 Jun 28.

PMID:
18625557
27.

Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.

Fish PV, Barta NS, Gray DL, Ryckmans T, Stobie A, Wakenhut F, Whitlock GA.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4355-9. doi: 10.1016/j.bmcl.2008.06.071. Epub 2008 Jun 25.

PMID:
18621528
28.

Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity.

Whitlock GA, Fish PV, Fray MJ, Stobie A, Wakenhut F.

Bioorg Med Chem Lett. 2008 May 1;18(9):2896-9. doi: 10.1016/j.bmcl.2008.03.082. Epub 2008 Apr 8.

PMID:
18417343
29.

Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition.

Fish PV, Deur C, Gan X, Greene K, Hoople D, Mackenny M, Para KS, Reeves K, Ryckmans T, Stiff C, Stobie A, Wakenhut F, Whitlock GA.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2562-6. doi: 10.1016/j.bmcl.2008.03.050. Epub 2008 Mar 20.

PMID:
18387300
30.

[4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors.

Fish PV, Ryckmans T, Stobie A, Wakenhut F.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1795-8. doi: 10.1016/j.bmcl.2008.02.036. Epub 2008 Feb 16.

PMID:
18313294
31.
32.

Potent and selective nonpeptidic inhibitors of procollagen C-proteinase.

Fish PV, Allan GA, Bailey S, Blagg J, Butt R, Collis MG, Greiling D, James K, Kendall J, McElroy A, McCleverty D, Reed C, Webster R, Whitlock GA.

J Med Chem. 2007 Jul 26;50(15):3442-56. Epub 2007 Jun 26.

PMID:
17591762
33.

Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines.

Fish PV, Barber CG, Brown DG, Butt R, Collis MG, Dickinson RP, Henry BT, Horne VA, Huggins JP, King E, O'Gara M, McCleverty D, McIntosh F, Phillips C, Webster R.

J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.

PMID:
17447747
34.

N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.

Fish PV, Fray MJ, Stobie A, Wakenhut F, Whitlock GA.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):2022-5. Epub 2007 Jan 19.

PMID:
17267217
35.

Predicting penetration across the blood-brain barrier from simple descriptors and fragmentation schemes.

Zhao YH, Abraham MH, Ibrahim A, Fish PV, Cole S, Lewis ML, de Groot MJ, Reynolds DP.

J Chem Inf Model. 2007 Jan-Feb;47(1):170-5.

PMID:
17238262
36.

Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.

Fray MJ, Bish G, Fish PV, Stobie A, Wakenhut F, Whitlock GA.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4349-53. Epub 2006 Jun 5.

PMID:
16750363
37.

N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.

Jonathan Fray M, Bish G, Brown AD, Fish PV, Stobie A, Wakenhut F, Whitlock GA.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4345-8. Epub 2006 Jun 5.

PMID:
16750359
38.

Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.

Barber CG, Dickinson RP, Fish PV.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.

PMID:
15149680
39.

Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence.

Danilewicz JC, Abel SM, Brown AD, Fish PV, Hawkeswood E, Holland SJ, James K, McElroy AB, Overington J, Powling MJ, Rance DJ.

J Med Chem. 2002 Jun 6;45(12):2432-53.

PMID:
12036353

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