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Items: 1 to 20 of 28

1.

Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis.

Hong WD, Gibbons PD, Leung SC, Amewu R, Stocks PA, Stachulski A, Horta P, Cristiano MLS, Shone AE, Moss D, Ardrey A, Sharma R, Warman AJ, Bedingfield PTP, Fisher NE, Aljayyoussi G, Mead S, Caws M, Berry NG, Ward SA, Biagini GA, O'Neill PM, Nixon GL.

J Med Chem. 2017 May 11;60(9):3703-3726. doi: 10.1021/acs.jmedchem.6b01718. Epub 2017 Apr 25.

2.

Novel inhibitors of the Plasmodium falciparum electron transport chain.

Stocks PA, Barton V, Antoine T, Biagini GA, Ward SA, O'Neill PM.

Parasitology. 2014 Jan;141(1):50-65. doi: 10.1017/S0031182013001571. Review.

PMID:
24401337
3.

Artemisinin-polypyrrole conjugates: synthesis, DNA binding studies and preliminary antiproliferative evaluation.

La Pensée L, Sabbani S, Sharma R, Bhamra I, Shore E, Chadwick AE, Berry NG, Firman J, Araujo NC, Cabral L, Cristiano ML, Bateman C, Janneh O, Gavrila A, Wu YH, Hussain A, Ward SA, Stocks PA, Cosstick R, O'Neill PM.

ChemMedChem. 2013 May;8(5):709-18. doi: 10.1002/cmdc.201200536. Epub 2013 Mar 11.

PMID:
23495190
4.

Glutathione transport: a new role for PfCRT in chloroquine resistance.

Patzewitz EM, Salcedo-Sora JE, Wong EH, Sethia S, Stocks PA, Maughan SC, Murray JA, Krishna S, Bray PG, Ward SA, Müller S.

Antioxid Redox Signal. 2013 Sep 1;19(7):683-95. doi: 10.1089/ars.2012.4625. Epub 2012 Dec 20.

5.

Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria.

Biagini GA, Fisher N, Shone AE, Mubaraki MA, Srivastava A, Hill A, Antoine T, Warman AJ, Davies J, Pidathala C, Amewu RK, Leung SC, Sharma R, Gibbons P, Hong DW, Pacorel B, Lawrenson AS, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Stocks PA, Nixon GL, Chadwick J, Hemingway J, Delves MJ, Sinden RE, Zeeman AM, Kocken CH, Berry NG, O'Neill PM, Ward SA.

Proc Natl Acad Sci U S A. 2012 May 22;109(21):8298-303. doi: 10.1073/pnas.1205651109. Epub 2012 May 7.

6.

Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

Leung SC, Gibbons P, Amewu R, Nixon GL, Pidathala C, Hong WD, Pacorel B, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM.

J Med Chem. 2012 Mar 8;55(5):1844-57. doi: 10.1021/jm201184h. Epub 2012 Feb 24.

7.

Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

Pidathala C, Amewu R, Pacorel B, Nixon GL, Gibbons P, Hong WD, Leung SC, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM.

J Med Chem. 2012 Mar 8;55(5):1831-43. doi: 10.1021/jm201179h. Epub 2012 Feb 24.

8.

The molecular basis of folate salvage in Plasmodium falciparum: characterization of two folate transporters.

Salcedo-Sora JE, Ochong E, Beveridge S, Johnson D, Nzila A, Biagini GA, Stocks PA, O'Neill PM, Krishna S, Bray PG, Ward SA.

J Biol Chem. 2011 Dec 30;286(52):44659-68. doi: 10.1074/jbc.M111.286054. Epub 2011 Oct 13.

9.

Antimalarial mannoxanes: hybrid antimalarial drugs with outstanding oral activity profiles and a potential dual mechanism of action.

Chadwick J, Amewu RK, Marti F, Garah FB, Sharma R, Berry NG, Stocks PA, Burrell-Saward H, Wittlin S, Rottmann M, Brun R, Taramelli D, Parapini S, Ward SA, O'Neill PM.

ChemMedChem. 2011 Aug 1;6(8):1357-61. doi: 10.1002/cmdc.201100196. Epub 2011 Jun 20. No abstract available.

PMID:
21692184
10.

Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity.

Gibbons P, Verissimo E, Araujo NC, Barton V, Nixon GL, Amewu RK, Chadwick J, Stocks PA, Biagini GA, Srivastava A, Rosenthal PJ, Gut J, Guedes RC, Moreira R, Sharma R, Berry N, Cristiano ML, Shone AE, Ward SA, O'Neill PM.

J Med Chem. 2010 Nov 25;53(22):8202-6. doi: 10.1021/jm1009567. Epub 2010 Oct 27.

PMID:
20979352
11.

Synthesis, in vitro and in vivo antimalarial assessment of sulfide, sulfone and vinyl amide-substituted 1,2,4-trioxanes prepared via thiol-olefin co-oxygenation (TOCO) of allylic alcohols.

Amewu R, Gibbons P, Mukhtar A, Stachulski AV, Ward SA, Hall C, Rimmer K, Davies J, Vivas L, Bacsa J, Mercer AE, Nixon G, Stocks PA, O'Neill PM.

Org Biomol Chem. 2010 May 7;8(9):2068-77. doi: 10.1039/b924319d. Epub 2010 Mar 3.

PMID:
20401383
12.

Design, synthesis and antimalarial/anticancer evaluation of spermidine linked artemisinin conjugates designed to exploit polyamine transporters in Plasmodium falciparum and HL-60 cancer cell lines.

Chadwick J, Jones M, Mercer AE, Stocks PA, Ward SA, Park BK, O'Neill PM.

Bioorg Med Chem. 2010 Apr 1;18(7):2586-97. doi: 10.1016/j.bmc.2010.02.035. Epub 2010 Feb 23.

PMID:
20227283
13.

Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.

O'Neill PM, Shone AE, Stanford D, Nixon G, Asadollahy E, Park BK, Maggs JL, Roberts P, Stocks PA, Biagini G, Bray PG, Davies J, Berry N, Hall C, Rimmer K, Winstanley PA, Hindley S, Bambal RB, Davis CB, Bates M, Gresham SL, Brigandi RA, Gomez-de-Las-Heras FM, Gargallo DV, Parapini S, Vivas L, Lander H, Taramelli D, Ward SA.

J Med Chem. 2009 Apr 9;52(7):1828-44. doi: 10.1021/jm8012757.

14.

Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.

Araújo NC, Barton V, Jones M, Stocks PA, Ward SA, Davies J, Bray PG, Shone AE, Cristiano ML, O'Neill PM.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):2038-43. doi: 10.1016/j.bmcl.2009.02.013. Epub 2009 Feb 8.

PMID:
19251414
15.

Antitumour and antimalarial activity of artemisinin-acridine hybrids.

Jones M, Mercer AE, Stocks PA, La Pensée LJ, Cosstick R, Park BK, Kennedy ME, Piantanida I, Ward SA, Davies J, Bray PG, Rawe SL, Baird J, Charidza T, Janneh O, O'Neill PM.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):2033-7. doi: 10.1016/j.bmcl.2009.02.028. Epub 2009 Feb 11.

PMID:
19249201
16.

Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.

O'Neill PM, Park BK, Shone AE, Maggs JL, Roberts P, Stocks PA, Biagini GA, Bray PG, Gibbons P, Berry N, Winstanley PA, Mukhtar A, Bonar-Law R, Hindley S, Bambal RB, Davis CB, Bates M, Hart TK, Gresham SL, Lawrence RM, Brigandi RA, Gomez-delas-Heras FM, Gargallo DV, Ward SA.

J Med Chem. 2009 Mar 12;52(5):1408-15. doi: 10.1021/jm8012618.

PMID:
19222165
17.

Piperidine dispiro-1,2,4-trioxane analogues.

Sabbani S, Stocks PA, Ellis GL, Davies J, Hedenstrom E, Ward SA, O'Neill PM.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5804-8. doi: 10.1016/j.bmcl.2008.09.052. Epub 2008 Sep 17.

PMID:
18845438
18.

Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.

Ellis GL, Amewu R, Sabbani S, Stocks PA, Shone A, Stanford D, Gibbons P, Davies J, Vivas L, Charnaud S, Bongard E, Hall C, Rimmer K, Lozanom S, Jesús M, Gargallo D, Ward SA, O'Neill PM.

J Med Chem. 2008 Apr 10;51(7):2170-7. doi: 10.1021/jm701435h. Epub 2008 Mar 15.

PMID:
18341274
19.

Acridinediones: selective and potent inhibitors of the malaria parasite mitochondrial bc1 complex.

Biagini GA, Fisher N, Berry N, Stocks PA, Meunier B, Williams DP, Bonar-Law R, Bray PG, Owen A, O'Neill PM, Ward SA.

Mol Pharmacol. 2008 May;73(5):1347-55. doi: 10.1124/mol.108.045120. Epub 2008 Mar 4.

20.

Evidence for a common non-heme chelatable-iron-dependent activation mechanism for semisynthetic and synthetic endoperoxide antimalarial drugs.

Stocks PA, Bray PG, Barton VE, Al-Helal M, Jones M, Araujo NC, Gibbons P, Ward SA, Hughes RH, Biagini GA, Davies J, Amewu R, Mercer AE, Ellis G, O'Neill PM.

Angew Chem Int Ed Engl. 2007;46(33):6278-83. No abstract available.

PMID:
17640025

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