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Items: 1 to 50 of 78

1.

In vitro efficacies, ADME, and pharmacokinetic properties of phenoxazine derivatives active against Mycobacterium tuberculosis.

Tanner L, Evans JC, Seldon R, Jordaan A, Warner DF, Haynes RK, Parkinson CJ, Wiesner L.

Antimicrob Agents Chemother. 2019 Aug 19. pii: AAC.01010-19. doi: 10.1128/AAC.01010-19. [Epub ahead of print]

PMID:
31427302
2.

Development of pyridyl thiosemicarbazones as highly potent agents for the treatment of malaria after oral administration.

Parkinson CJ, Birrell GW, Chavchich M, Mackenzie D, Haynes RK, de Kock C, Richardson DR, Edstein MD.

J Antimicrob Chemother. 2019 Jul 19. pii: dkz290. doi: 10.1093/jac/dkz290. [Epub ahead of print]

PMID:
31325302
3.

Anti-Mycobacterial Peroxides: A new class of agents for development against tuberculosis.

van der Westhuyzen CW, Haynes RK, Panayides JL, Wiid I, Parkinson CJ.

Med Chem. 2019 Apr 30. doi: 10.2174/1573406415666190430143535. [Epub ahead of print]

PMID:
31208310
4.

An in vitro ADME and in vivo Pharmacokinetic Study of Novel TB-Active Decoquinate Derivatives.

Tanner L, Haynes RK, Wiesner L.

Front Pharmacol. 2019 Feb 18;10:120. doi: 10.3389/fphar.2019.00120. eCollection 2019.

5.

The evaluation of the anti-cancer drug elesclomol that forms a redox-active copper chelate as a potential anti-tubercular drug.

Ngwane AH, Petersen RD, Baker B, Wiid I, Wong HN, Haynes RK.

IUBMB Life. 2019 May;71(5):532-538. doi: 10.1002/iub.2002. Epub 2019 Jan 14.

PMID:
30698324
6.

Topical Delivery of Artemisone, Clofazimine and Decoquinate Encapsulated in Vesicles and Their In vitro Efficacy Against Mycobacterium tuberculosis.

van Zyl L, Viljoen JM, Haynes RK, Aucamp M, Ngwane AH, du Plessis J.

AAPS PharmSciTech. 2019 Jan 2;20(1):33. doi: 10.1208/s12249-018-1251-5.

PMID:
30604176
7.

Synthesis, antimalarial activities and cytotoxicities of amino-artemisinin-1,2-disubstituted ferrocene hybrids.

de Lange C, Coertzen D, Smit FJ, Wentzel JF, Wong HN, Birkholtz LM, Haynes RK, N'Da DD.

Bioorg Med Chem Lett. 2018 Oct 15;28(19):3161-3163. doi: 10.1016/j.bmcl.2018.08.037. Epub 2018 Aug 28.

PMID:
30174153
8.

Corrigendum to 'In vitro activity of artemisone and artemisinin derivatives against extracellular and intracellular Helicobacter pylori' [International Journal of Antimicrobial Agents 48/1 (2016) 101-105].

Sisto F, Scaltrito MM, Masia C, Bonomi A, Coccè V, Marano G, Haynes RK, Miani A, Farronato G, Taramelli D.

Int J Antimicrob Agents. 2018 Oct;52(4):528. doi: 10.1016/j.ijantimicag.2018.08.006. Epub 2018 Aug 30. No abstract available.

PMID:
30172701
9.

Formulation of Natural Oil Nano-Emulsions for the Topical Delivery of Clofazimine, Artemisone and Decoquinate.

Burger C, Aucamp M, du Preez J, Haynes RK, Ngwane A, du Plessis J, Gerber M.

Pharm Res. 2018 Aug 7;35(10):186. doi: 10.1007/s11095-018-2471-9.

PMID:
30088097
10.

Facile Preparation of N-Glycosylated 10-Piperazinyl Artemisinin Derivatives and Evaluation of Their Antimalarial and Cytotoxic Activities.

Wu Y, Parapini S, Williams ID, Misiano P, Wong HN, Taramelli D, Basilico N, Haynes RK.

Molecules. 2018 Jul 13;23(7). pii: E1713. doi: 10.3390/molecules23071713.

11.

Cocrystals of the antimalarial drug 11-azaartemisinin with three alkenoic acids of 1:1 or 2:1 stoichiometry.

Nisar M, Wong LWY, Sung HHY, Haynes RK, Williams ID.

Acta Crystallogr C Struct Chem. 2018 Jun 1;74(Pt 6):742-751. doi: 10.1107/S2053229618006320. Epub 2018 May 24.

PMID:
29870011
12.

Artemisone and Artemiside Are Potent Panreactive Antimalarial Agents That Also Synergize Redox Imbalance in Plasmodium falciparum Transmissible Gametocyte Stages.

Coertzen D, Reader J, van der Watt M, Nondaba SH, Gibhard L, Wiesner L, Smith P, D'Alessandro S, Taramelli D, Wong HN, du Preez JL, Wu RWK, Birkholtz LM, Haynes RK.

Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e02214-17. doi: 10.1128/AAC.02214-17. Print 2018 Aug.

13.

The Evaluation of Metal Co-ordinating Bis-Thiosemicarbazones as Potential Anti-malarial Agents.

Akladios FN, Andrew SD, Boog SJ, de Kock C, Haynes RK, Parkinson CJ.

Med Chem. 2019;15(1):51-58. doi: 10.2174/1573406414666180525132204.

PMID:
29804537
14.

Absorptive and Secretory Transport of Selected Artemisinin Derivatives Across Caco-2 Cell Monolayers.

Heyns J, Willers C, Haynes RK, Wong HN, Hamman J, Gouws C.

Curr Drug Deliv. 2018;15(8):1183-1192. doi: 10.2174/1567201815666180518125113.

PMID:
29779481
15.

The Artemisinin Derivative Artemisone Is a Potent Inhibitor of Human Cytomegalovirus Replication.

Oiknine-Djian E, Weisblum Y, Panet A, Wong HN, Haynes RK, Wolf DG.

Antimicrob Agents Chemother. 2018 Jun 26;62(7). pii: e00288-18. doi: 10.1128/AAC.00288-18. Print 2018 Jul.

16.

Synthesis, in vitro antimalarial activities and cytotoxicities of amino-artemisinin-ferrocene derivatives.

de Lange C, Coertzen D, Smit FJ, Wentzel JF, Wong HN, Birkholtz LM, Haynes RK, N'Da DD.

Bioorg Med Chem Lett. 2018 Feb 1;28(3):289-292. doi: 10.1016/j.bmcl.2017.12.057. Epub 2017 Dec 26.

PMID:
29317166
17.

Activities of 11-Azaartemisinin and N-Sulfonyl Derivatives against Asexual and Transmissible Malaria Parasites.

Harmse R, Coertzen D, Wong HN, Smit FJ, van der Watt ME, Reader J, Nondaba SH, Birkholtz LM, Haynes RK, N'Da DD.

ChemMedChem. 2017 Dec 19;12(24):2086-2093. doi: 10.1002/cmdc.201700599. Epub 2017 Dec 8.

PMID:
29219249
18.

Activities of 11-Azaartemisinin and N-Sulfonyl Derivatives against Neospora caninum and Comparative Cytotoxicities.

Harmse R, Wong HN, Smit FJ, Müller J, Hemphill A, N'Da DD, Haynes RK.

ChemMedChem. 2017 Dec 19;12(24):2094-2098. doi: 10.1002/cmdc.201700600. Epub 2017 Dec 6.

PMID:
29210523
19.

Preliminary Evaluation of Artemisinin-Cholesterol Conjugates as Potential Drugs for the Treatment of Intractable Forms of Malaria and Tuberculosis.

Morake M, Coertzen D, Ngwane A, Wentzel JF, Wong HN, Smit FJ, Birkholtz LM, Pietersen RD, Baker B, Wiid I, N'Da DD, Haynes RK.

ChemMedChem. 2018 Jan 8;13(1):67-77. doi: 10.1002/cmdc.201700579. Epub 2017 Dec 15.

PMID:
29193799
20.

Elimination of Schistosoma mansoni in infected mice by slow release of artemisone.

Gold D, Alian M, Domb A, Karawani Y, Jbarien M, Chollet J, Haynes RK, Wong HN, Buchholz V, Greiner A, Golenser J.

Int J Parasitol Drugs Drug Resist. 2017 Aug;7(2):241-247. doi: 10.1016/j.ijpddr.2017.05.002. Epub 2017 May 4.

21.

Methylene Homologues of Artemisone: An Unexpected Structure-Activity Relationship and a Possible Implication for the Design of C10-Substituted Artemisinins.

Wu Y, Wu RW, Cheu KW, Williams ID, Krishna S, Slavic K, Gravett AM, Liu WM, Wong HN, Haynes RK.

ChemMedChem. 2016 Jul 5;11(13):1469-79. doi: 10.1002/cmdc.201600011. Epub 2016 Jun 7.

PMID:
27273875
22.

In vitro activity of artemisone and artemisinin derivatives against extracellular and intracellular Helicobacter pylori.

Sisto F, Scaltrito MM, Masia C, Bonomi A, Coccè V, Marano G, Haynes RK, Miani A, Farronato G, Taramelli D.

Int J Antimicrob Agents. 2016 Jul;48(1):101-105. doi: 10.1016/j.ijantimicag.2016.03.018. Epub 2016 May 6. Erratum in: Int J Antimicrob Agents. 2018 Oct;52(4):528.

PMID:
27216383
23.

Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities.

Beteck RM, Coertzen D, Smit FJ, Birkholtz LM, Haynes RK, N'Da DD.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):3006-3009. doi: 10.1016/j.bmcl.2016.05.024. Epub 2016 May 9.

PMID:
27210430
24.

In vitro skin permeation of artemisone and its nano-vesicular formulations.

Dwivedi A, Mazumder A, Fox LT, Brümmer A, Gerber M, du Preez JL, Haynes RK, du Plessis J.

Int J Pharm. 2016 Apr 30;503(1-2):1-7. doi: 10.1016/j.ijpharm.2016.02.041. Epub 2016 Feb 27.

PMID:
26930566
25.

Repurposing of antiparasitic drugs: the hydroxy-naphthoquinone buparvaquone inhibits vertical transmission in the pregnant neosporosis mouse model.

Müller J, Aguado-Martínez A, Manser V, Wong HN, Haynes RK, Hemphill A.

Vet Res. 2016 Feb 17;47:32. doi: 10.1186/s13567-016-0317-1.

26.

In vitro anti-cancer effects of artemisone nano-vesicular formulations on melanoma cells.

Dwivedi A, Mazumder A, du Plessis L, du Preez JL, Haynes RK, du Plessis J.

Nanomedicine. 2015 Nov;11(8):2041-50. doi: 10.1016/j.nano.2015.07.010. Epub 2015 Aug 15.

PMID:
26282380
27.

The Case for Development of 11-Aza-artemisinins for Malaria.

Harmse R, Wong HN, Smit F, Haynes RK, N'Da DD.

Curr Med Chem. 2015;22(31):3607-30. Review.

PMID:
26219389
28.

In vitro effects of new artemisinin derivatives in Neospora caninum-infected human fibroblasts.

Müller J, Balmer V, Winzer P, Rahman M, Manser V, Haynes RK, Hemphill A.

Int J Antimicrob Agents. 2015 Jul;46(1):88-93. doi: 10.1016/j.ijantimicag.2015.02.020. Epub 2015 Apr 14.

PMID:
25934265
29.

Assessment of the induction of dormant ring stages in Plasmodium falciparum parasites by artemisone and artemisone entrapped in Pheroid vesicles in vitro.

Grobler L, Chavchich M, Haynes RK, Edstein MD, Grobler AF.

Antimicrob Agents Chemother. 2014 Dec;58(12):7579-82. doi: 10.1128/AAC.02707-14. Epub 2014 Oct 6.

30.

Recent progress in the development of anti-malarial quinolones.

Beteck RM, Smit FJ, Haynes RK, N'Da DD.

Malar J. 2014 Aug 30;13:339. doi: 10.1186/1475-2875-13-339. Review.

31.

Inhibition of metalloproteinase-9 secretion and gene expression by artemisinin derivatives.

Magenta D, Sangiovanni E, Basilico N, Haynes RK, Parapini S, Colombo E, Bosisio E, Taramelli D, Dell'Agli M.

Acta Trop. 2014 Dec;140:77-83. doi: 10.1016/j.actatropica.2014.08.008. Epub 2014 Aug 19.

PMID:
25149353
32.

Treatment of murine cerebral malaria by artemisone in combination with conventional antimalarial drugs: antiplasmodial effects and immune responses.

Guiguemde WA, Hunt NH, Guo J, Marciano A, Haynes RK, Clark J, Guy RK, Golenser J.

Antimicrob Agents Chemother. 2014 Aug;58(8):4745-54. doi: 10.1128/AAC.01553-13. Epub 2014 Jun 9.

33.

Anticancer properties of distinct antimalarial drug classes.

Hooft van Huijsduijnen R, Guy RK, Chibale K, Haynes RK, Peitz I, Kelter G, Phillips MA, Vennerstrom JL, Yuthavong Y, Wells TN.

PLoS One. 2013 Dec 31;8(12):e82962. doi: 10.1371/journal.pone.0082962. eCollection 2013.

34.

Considerations on the mechanism of action of artemisinin antimalarials: part 1--the 'carbon radical' and 'heme' hypotheses.

Haynes RK, Cheu KW, N'Da D, Coghi P, Monti D.

Infect Disord Drug Targets. 2013 Aug;13(4):217-77. Review.

PMID:
24304352
35.

Artemisone inhibits in vitro and in vivo propagation of Babesia bovis and B. bigemina parasites.

Mazuz ML, Golenser J, Fish L, Haynes RK, Wollkomirsky R, Leibovich B, Shkap V.

Exp Parasitol. 2013 Dec;135(4):690-4. doi: 10.1016/j.exppara.2013.10.006. Epub 2013 Oct 30.

PMID:
24184077
36.

Glucocorticosteroids in nano-sterically stabilized liposomes are efficacious for elimination of the acute symptoms of experimental cerebral malaria.

Waknine-Grinberg JH, Even-Chen S, Avichzer J, Turjeman K, Bentura-Marciano A, Haynes RK, Weiss L, Allon N, Ovadia H, Golenser J, Barenholz Y.

PLoS One. 2013 Aug 26;8(8):e72722. doi: 10.1371/journal.pone.0072722. eCollection 2013.

37.

Expression in yeast links field polymorphisms in PfATP6 to in vitro artemisinin resistance and identifies new inhibitor classes.

Pulcini S, Staines HM, Pittman JK, Slavic K, Doerig C, Halbert J, Tewari R, Shah F, Avery MA, Haynes RK, Krishna S.

J Infect Dis. 2013 Aug 1;208(3):468-78. doi: 10.1093/infdis/jit171. Epub 2013 Apr 18.

PMID:
23599312
38.

Interactions between artemisinins and other antimalarial drugs in relation to the cofactor model--a unifying proposal for drug action.

Haynes RK, Cheu KW, Chan HW, Wong HN, Li KY, Tang MM, Chen MJ, Guo ZF, Guo ZH, Sinniah K, Witte AB, Coghi P, Monti D.

ChemMedChem. 2012 Dec;7(12):2204-26. doi: 10.1002/cmdc.201200383. Epub 2012 Oct 30.

PMID:
23112085
39.

Comparative ex vivo activity of novel endoperoxides in multidrug-resistant plasmodium falciparum and P. vivax.

Marfurt J, Chalfein F, Prayoga P, Wabiser F, Wirjanata G, Sebayang B, Piera KA, Wittlin S, Haynes RK, Möhrle JJ, Anstey NM, Kenangalem E, Price RN.

Antimicrob Agents Chemother. 2012 Oct;56(10):5258-63. doi: 10.1128/AAC.00283-12. Epub 2012 Jul 30.

40.

Dihydroartemisinin inhibits the human erythroid cell differentiation by altering the cell cycle.

Finaurini S, Basilico N, Corbett Y, D'Alessandro S, Parapini S, Olliaro P, Haynes RK, Taramelli D.

Toxicology. 2012 Oct 9;300(1-2):57-66. doi: 10.1016/j.tox.2012.05.024. Epub 2012 Jun 5.

PMID:
22677887
41.

Synthesis of artemiside and its effects in combination with conventional drugs against severe murine malaria.

Guo J, Guiguemde AW, Bentura-Marciano A, Clark J, Haynes RK, Chan WC, Wong HN, Hunt NH, Guy RK, Golenser J.

Antimicrob Agents Chemother. 2012 Jan;56(1):163-73. doi: 10.1128/AAC.05006-11. Epub 2011 Oct 17.

42.

A partial convergence in action of methylene blue and artemisinins: antagonism with chloroquine, a reversal with verapamil, and an insight into the antimalarial activity of chloroquine.

Haynes RK, Cheu KW, Li KY, Tang MM, Wong HN, Chen MJ, Guo ZF, Guo ZH, Coghi P, Monti D.

ChemMedChem. 2011 Sep 5;6(9):1603-15. doi: 10.1002/cmdc.201100184. Epub 2011 Jul 11.

PMID:
21994127
43.

Absorption of the novel artemisinin derivatives artemisone and artemiside: potential application of Pheroid™ technology.

Steyn JD, Wiesner L, du Plessis LH, Grobler AF, Smith PJ, Chan WC, Haynes RK, Kotzé AF.

Int J Pharm. 2011 Jul 29;414(1-2):260-6. doi: 10.1016/j.ijpharm.2011.05.003. Epub 2011 May 7.

PMID:
21596127
44.

Reactions of antimalarial peroxides with each of leucomethylene blue and dihydroflavins: flavin reductase and the cofactor model exemplified.

Haynes RK, Cheu KW, Tang MM, Chen MJ, Guo ZF, Guo ZH, Coghi P, Monti D.

ChemMedChem. 2011 Feb 7;6(2):279-91. doi: 10.1002/cmdc.201000508. Epub 2010 Dec 23.

PMID:
21275052
45.

Artemisone uptake in Plasmodium falciparum-infected erythrocytes.

Pooley S, Fatih FA, Krishna S, Gerisch M, Haynes RK, Wong HN, Staines HM.

Antimicrob Agents Chemother. 2011 Feb;55(2):550-6. doi: 10.1128/AAC.01216-10. Epub 2010 Dec 6.

46.

Artemisone effective against murine cerebral malaria.

Waknine-Grinberg JH, Hunt N, Bentura-Marciano A, McQuillan JA, Chan HW, Chan WC, Barenholz Y, Haynes RK, Golenser J.

Malar J. 2010 Aug 9;9:227. doi: 10.1186/1475-2875-9-227.

47.

Facile oxidation of leucomethylene blue and dihydroflavins by artemisinins: relationship with flavoenzyme function and antimalarial mechanism of action.

Haynes RK, Chan WC, Wong HN, Li KY, Wu WK, Fan KM, Sung HH, Williams ID, Prosperi D, Melato S, Coghi P, Monti D.

ChemMedChem. 2010 Aug 2;5(8):1282-99. doi: 10.1002/cmdc.201000225.

PMID:
20629071
48.

In vitro study of the anti-cancer effects of artemisone alone or in combination with other chemotherapeutic agents.

Gravett AM, Liu WM, Krishna S, Chan WC, Haynes RK, Wilson NL, Dalgleish AG.

Cancer Chemother Pharmacol. 2011 Mar;67(3):569-77. doi: 10.1007/s00280-010-1355-4. Epub 2010 May 19.

PMID:
20490800
49.

Interaction of artemisinins with oxyhemoglobin Hb-FeII, Hb-FeII, carboxyHb-FeII, heme-FeII, and carboxyheme FeII: significance for mode of action and implications for therapy of cerebral malaria.

Coghi P, Basilico N, Taramelli D, Chan WC, Haynes RK, Monti D.

ChemMedChem. 2009 Dec;4(12):2045-53. doi: 10.1002/cmdc.200900342.

PMID:
19844934
50.

Artemisone and artemiside control acute and reactivated toxoplasmosis in a murine model.

Dunay IR, Chan WC, Haynes RK, Sibley LD.

Antimicrob Agents Chemother. 2009 Oct;53(10):4450-6. doi: 10.1128/AAC.00502-09. Epub 2009 Jul 27.

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