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Items: 15


The palladacycle complex AJ-5 induces apoptotic cell death while reducing autophagic flux in rhabdomyosarcoma cells.

Bleloch JS, du Toit A, Gibhard L, Kimani S, Ballim RD, Lee M, Blanckenberg A, Mapolie S, Wiesner L, Loos B, Prince S.

Cell Death Discov. 2019 Jan 28;5:60. doi: 10.1038/s41420-019-0139-9. eCollection 2019.


Structure-Activity Relationship Studies and Plasmodium Life Cycle Profiling Identifies Pan-Active N-Aryl-3-trifluoromethyl Pyrido[1,2- a]benzimidazoles Which Are Efficacious in an in Vivo Mouse Model of Malaria.

Mayoka G, Njoroge M, Okombo J, Gibhard L, Sanches-Vaz M, Fontinha D, Birkholtz LM, Reader J, van der Watt M, Coetzer TL, Lauterbach S, Churchyard A, Bezuidenhout B, Egan TJ, Yeates C, Wittlin S, Prudêncio M, Chibale K.

J Med Chem. 2019 Jan 24;62(2):1022-1035. doi: 10.1021/acs.jmedchem.8b01769. Epub 2018 Dec 24.


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.


Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria.

Gibhard L, Njoroge M, Paquet T, Brunschwig C, Taylor D, Lawrence N, Abay E, Wittlin S, Wiesner L, Street LJ, Chibale K, Basarab GS.

Antimicrob Agents Chemother. 2018 Nov 26;62(12). pii: e00261-18. doi: 10.1128/AAC.00261-18. Print 2018 Dec.


Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.

Kandepedu N, Gonzàlez Cabrera D, Eedubilli S, Taylor D, Brunschwig C, Gibhard L, Njoroge M, Lawrence N, Paquet T, Eyermann CJ, Spangenberg T, Basarab GS, Street LJ, Chibale K.

J Med Chem. 2018 Jul 12;61(13):5692-5703. doi: 10.1021/acs.jmedchem.8b00648. Epub 2018 Jun 27.


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.


Antischistosomal Activity of Pyrido[1,2-a]benzimidazole Derivatives and Correlation with Inhibition of β-Hematin Formation.

Okombo J, Singh K, Mayoka G, Ndubi F, Barnard L, Njogu PM, Njoroge M, Gibhard L, Brunschwig C, Vargas M, Keiser J, Egan TJ, Chibale K.

ACS Infect Dis. 2017 Jun 9;3(6):411-420. doi: 10.1021/acsinfecdis.6b00205. Epub 2017 May 3.


In Vitro and In Vivo Pharmacokinetics of Aminoalkylated Diarylpropanes NP085 and NP102.

Gibhard L, Pravin K, Abay E, Wilhelm A, Swart K, Lawrence N, Khoury R, van der Westhuizen J, Smith P, Wiesner L.

Antimicrob Agents Chemother. 2016 Apr 22;60(5):3065-9. doi: 10.1128/AAC.02104-15. Print 2016 May.


Optimization of a multi-well colorimetric assay to determine haem species in Plasmodium falciparum in the presence of anti-malarials.

Combrinck JM, Fong KY, Gibhard L, Smith PJ, Wright DW, Egan TJ.

Malar J. 2015 Jun 24;14:253. doi: 10.1186/s12936-015-0729-9.


Oral lipid-based nanoformulation of tafenoquine enhanced bioavailability and blood stage antimalarial efficacy and led to a reduction in human red blood cell loss in mice.

Melariri P, Kalombo L, Nkuna P, Dube A, Hayeshi R, Ogutu B, Gibhard L, deKock C, Smith P, Wiesner L, Swai H.

Int J Nanomedicine. 2015 Feb 20;10:1493-503. doi: 10.2147/IJN.S76317. eCollection 2015.


Development and validation of a LC-MS/MS method for the quantitation of lumefantrine in mouse whole blood and plasma.

Govender K, Gibhard L, Du Plessis L, Wiesner L.

J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Mar 15;985:6-13. doi: 10.1016/j.jchromb.2015.01.015. Epub 2015 Jan 21.


Efficacy and pharmacokinetic evaluation of a novel anti-malarial compound (NP046) in a mouse model.

Abay ET, van der Westuizen JH, Swart KJ, Gibhard L, Lawrence N, Dambuza N, Wilhelm A, Pravin K, Wiesner L.

Malar J. 2015 Jan 6;14:8. doi: 10.1186/1475-2875-14-8.


Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds.

Tukulula M, Njoroge M, Abay ET, Mugumbate GC, Wiesner L, Taylor D, Gibhard L, Norman J, Swart KJ, Gut J, Rosenthal PJ, Barteau S, Streckfuss J, Kameni-Tcheudji J, Chibale K.

ACS Med Chem Lett. 2013 Oct 1;4(12):1198-202. doi: 10.1021/ml400311r. eCollection 2013 Dec 12.


Pharmacokinetic evaluation of lisinopril-tryptophan, a novel C-domain ACE inhibitor.

Denti P, Sharp SK, Kröger WL, Schwager SL, Mahajan A, Njoroge M, Gibhard L, Smit I, Chibale K, Wiesner L, Sturrock ED, Davies NH.

Eur J Pharm Sci. 2014 Jun 2;56:113-9. doi: 10.1016/j.ejps.2014.01.012. Epub 2014 Feb 20.


The development and validation of an LC-MS/MS method for the determination of a new anti-malarial compound (TK900D) in human whole blood and its application to pharmacokinetic studies in mice.

Abay ET, van der Westhuizen JH, Swart KJ, Gibhard L, Tukulula M, Chibale K, Wiesner L.

Malar J. 2014 Jan 31;13:42. doi: 10.1186/1475-2875-13-42.

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