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Items: 19

1.

Optimisation of a key cross-coupling reaction towards the synthesis of a promising antileishmanial compound.

Velasco RF, Guerrero C, Fra G, Moure A, Miguel-Siles J, Quesada-Campos MT, Ruiz-Gomez JR, Gilbert IH, Thomas MG, Miles TJ.

Tetrahedron Lett. 2019 May 2;60(18):1243-1247. doi: 10.1016/j.tetlet.2019.03.068.

2.

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.

3.

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.

4.

Short-Term Outcomes of Concussions in Major League Baseball: A Historical Cohort Study of Return to Play, Performance, Longevity, and Financial Impact.

Ramkumar PN, Navarro SM, Haeberle HS, Pettit RW, Miles TJ, Frangiamore SJ, Mont MA, Farrow LD, Schickendantz MS.

Orthop J Sports Med. 2018 Dec 13;6(12):2325967118814238. doi: 10.1177/2325967118814238. eCollection 2018 Dec.

5.

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
6.

Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis.

Wyllie S, Thomas M, Patterson S, Crouch S, De Rycker M, Lowe R, Gresham S, Urbaniak MD, Otto TD, Stojanovski L, Simeons FRC, Manthri S, MacLean LM, Zuccotto F, Homeyer N, Pflaumer H, Boesche M, Sastry L, Connolly P, Albrecht S, Berriman M, Drewes G, Gray DW, Ghidelli-Disse S, Dixon S, Fiandor JM, Wyatt PG, Ferguson MAJ, Fairlamb AH, Miles TJ, Read KD, Gilbert IH.

Nature. 2018 Aug;560(7717):192-197. doi: 10.1038/s41586-018-0356-z. Epub 2018 Jul 25.

7.

Antitrypanosomal 8-Hydroxy-Naphthyridines Are Chelators of Divalent Transition Metals.

Wall RJ, Moniz S, Thomas MG, Norval S, Ko EJ, Marco M, Miles TJ, Gilbert IH, Horn D, Fairlamb AH, Wyllie S.

Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e00235-18. doi: 10.1128/AAC.00235-18. Print 2018 Aug.

8.

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.

9.

Identification of Trypanocidal Activity for Known Clinical Compounds Using a New Trypanosoma cruzi Hit-Discovery Screening Cascade.

De Rycker M, Thomas J, Riley J, Brough SJ, Miles TJ, Gray DW.

PLoS Negl Trop Dis. 2016 Apr 15;10(4):e0004584. doi: 10.1371/journal.pntd.0004584. eCollection 2016 Apr.

10.

Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.

Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Jones GE, Kusalakumari Sukmar SK, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND.

Bioorg Med Chem Lett. 2016 May 15;26(10):2464-2469. doi: 10.1016/j.bmcl.2016.03.106. Epub 2016 Mar 31.

PMID:
27055939
11.

The teaching/research trade-off in law: data from the right tail.

Ginsburg T, Miles TJ.

Eval Rev. 2015 Feb;39(1):46-81. doi: 10.1177/0193841X14525173. Epub 2014 Mar 20. Review.

PMID:
24651660
12.

Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.

Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Huang J, Jones GE, Sukmar SK, Spitzfaden C, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5437-41. doi: 10.1016/j.bmcl.2013.07.013. Epub 2013 Jul 17.

PMID:
23968823
13.

Asymmetric synthesis of the fully elaborated pyrrolidinone core of oxazolomycin A.

Donohoe TJ, O'Riordan TJ, Peifer M, Jones CR, Miles TJ.

Org Lett. 2012 Nov 2;14(21):5460-3. doi: 10.1021/ol302541j. Epub 2012 Oct 12.

PMID:
23061613
14.

Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.

Miles TJ, Axten JM, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Gallagher T, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Miller WH, Minthorn EA, Rittenhouse S, Seefeld M, Pearson N.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7489-95. doi: 10.1016/j.bmcl.2011.09.117. Epub 2011 Oct 10.

PMID:
22047689
15.

Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.

Miles TJ, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Rittenhouse S, Xiang H, Pearson N.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7483-8. doi: 10.1016/j.bmcl.2011.09.114. Epub 2011 Oct 10.

PMID:
22030032
16.

Structural basis of quinolone inhibition of type IIA topoisomerases and target-mediated resistance.

Wohlkonig A, Chan PF, Fosberry AP, Homes P, Huang J, Kranz M, Leydon VR, Miles TJ, Pearson ND, Perera RL, Shillings AJ, Gwynn MN, Bax BD.

Nat Struct Mol Biol. 2010 Sep;17(9):1152-3. doi: 10.1038/nsmb.1892. Epub 2010 Aug 29.

PMID:
20802486
17.

Organolithium-induced alkylative ring opening of aziridines: synthesis of unsaturated amino alcohols and ethers.

Hodgson DM, Stefane B, Miles TJ, Witherington J.

J Org Chem. 2006 Oct 27;71(22):8510-5.

PMID:
17064027
18.

Unsaturated 1,2-amino alcohols and ethers from aziridines and organolithiums.

Hodgson DM, Stefane B, Miles TJ, Witherington J.

Chem Commun (Camb). 2004 Oct 7;(19):2234-5. Epub 2004 Aug 24.

PMID:
15467888
19.

Enantioselective alkylative double ring opening of epoxides: synthesis of enantioenriched unsaturated diols and amino alcohols.

Hodgson DM, Maxwell CR, Miles TJ, Paruch E, Stent MA, Matthews IR, Wilson FX, Witherington J.

Angew Chem Int Ed Engl. 2002 Nov 15;41(22):4313-6. No abstract available. Erratum in: Angew Chem Int Ed Engl. 2002 Dec 16;41(24):464.

PMID:
12434373

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