Search Results - "Ncokazi, Kanyile"

Insights into the Role of Heme in the Mechanism of Action of Antimalarials by Combrinck, Jill M, Mabotha, Tebogo E, Ncokazi, Kanyile K, Ambele, Melvin A, Taylor, Dale, Smith, Peter J, Hoppe, Heinrich C, Egan, Timothy J

“…By using cell fractionation and measurement of Fe­(III)­heme-pyridine, the antimalarial chloroquine (CQ) has been shown to cause a dose-dependent decrease in…”
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The Antimalarial Ferroquine: Role of the Metal and Intramolecular Hydrogen Bond in Activity and Resistance by Dubar, Faustine, Egan, Timothy J, Pradines, Bruno, Kuter, David, Ncokazi, Kanyile K, Forge, Delphine, Paul, Jean-François, Pierrot, Christine, Kalamou, Hadidjatou, Khalife, Jamal, Buisine, Eric, Rogier, Christophe, Vezin, Hervé, Forfar, Isabelle, Slomianny, Christian, Trivelli, Xavier, Kapishnikov, Sergey, Leiserowitz, Leslie, Dive, Daniel, Biot, Christophe

“…Inhibition of hemozoin biocrystallization is considered the main mechanism of action of 4-aminoquinoline antimalarials including chloroquine (CQ) but cannot…”
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A colorimetric high-throughput β-hematin inhibition screening assay for use in the search for antimalarial compounds by Ncokazi, Kanyile K., Egan, Timothy J.

“…Antimalarial drugs such as chloroquine are believed to act by inhibiting hemozoin formation in the food vacuole of the malaria parasite. We have developed a…”
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Haemozoin (β-haematin) biomineralization occurs by self-assembly near the lipid/water interface by Egan, Timothy J., Chen, Jeff Y-J., de Villiers, Katherine A., Mabotha, Tebogo E., Naidoo, Kevin J., Ncokazi, Kanyile K., Langford, Steven J., McNaughton, Don, Pandiancherri, Shveta, Wood, Bayden R.

“…Several blood-feeding organisms, including the malaria parasite detoxify haem released from host haemoglobin by conversion to the insoluble crystalline…”
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Crystallization of synthetic haemozoin (beta-haematin) nucleated at the surface of lipid particles by Hoang, Anh N, Ncokazi, Kanyile K, de Villiers, Katherine A, Wright, David W, Egan, Timothy J

“…The mechanism of formation of haemozoin, a detoxification by-product of several blood-feeding organisms including malaria parasites, has been a subject of…”
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Quinoline antimalarials decrease the rate of β-hematin formation by Egan, Timothy J., Ncokazi, Kanyile K.

“…The strength of inhibition of β-hematin (synthetic hemozoin or malaria pigment) formation by the quinoline antimalarial drugs chloroquine, amodiaquine,…”
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The Mechanism of β-Hematin Formation in Acetate Solution. Parallels between Hemozoin Formation and Biomineralization Processes by Egan, Timothy J, Mavuso, Winile W, Ncokazi, Kanyile K

“…Formation of β-hematin in acidic acetate solution has been investigated using quantitative infrared spectroscopy, X-ray diffraction, and scanning and…”
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Effects of solvent composition and ionic strength on the interaction of quinoline antimalarials with ferriprotoporphyrin IX by Egan, Timothy J, Ncokazi, Kanyile K

“…Enthalpy-entropy compensation in the interaction of quinoline antimalarials with ferriprotoporphyrin IX (Fe(III)PPIX) in 40% aqueous dimethyl sulfoxide (DMSO)…”
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Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds by Guantai, Eric M., Ncokazi, Kanyile, Egan, Timothy J., Gut, Jiri, Rosenthal, Philip J., Smith, Peter J., Chibale, Kelly

“…A targeted series of chalcone and dienone hybrid compounds containing aminoquinoline and nucleoside templates was synthesized and evaluated for in vitro…”
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Enone– and Chalcone–Chloroquinoline Hybrid Analogues: In Silico Guided Design, Synthesis, Antiplasmodial Activity, in Vitro Metabolism, and Mechanistic Studies by Guantai, Eric M, Ncokazi, Kanyile, Egan, Timothy J, Gut, Jiri, Rosenthal, Philip J, Bhampidipati, Ravi, Kopinathan, Anitha, Smith, Peter J, Chibale, Kelly

“…Analogues of the previously reported antimalarial hybrid compounds 8b and 12 were proposed with the aim of identifying compounds with improved solubility and…”
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Effects of highly active novel artemisinin–chloroquinoline hybrid compounds on β-hematin formation, parasite morphology and endocytosis in Plasmodium falciparum by Feng, Tzu-Shean, Guantai, Eric M., Nell, Margo, van Rensburg, Constance E.J., Ncokazi, Kanyile, Egan, Timothy J., Hoppe, Heinrich C., Chibale, Kelly

“…4-Aminoquinolines were hybridized with artemisinin and 1,4-naphthoquinone derivatives via the Ugi-four-component condensation reaction, and their biological…”
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Reversed Chloroquines Based on the 3,4‐Dihydropyrimidin‐2(1H)‐one Scaffold: Synthesis and Evaluation for Antimalarial, β‐Haematin Inhibition, and Cytotoxic Activity by October, Natasha, Watermeyer, Nicholas D., Yardley, Vanessa, Egan, Timothy J., Ncokazi, Kanyile, Chibale, Kelly

“…The synthesis, cytotoxicity, and antimalarial activity of resistance‐reversing bifunctional dihydropyrimidone–chloroquinoline conjugates are reported herein…”
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Antiplasmodial, beta-haematin inhibition, antitrypanosomal and cytotoxic activity in vitro of novel 4-aminoquinoline 2-imidazolines by Musonda, Chitalu C, Yardley, Vanessa, de Souza, Renata C Carvalho, Ncokazi, Kanyile, Egan, Timothy J, Chibale, Kelly

“…A novel series of 4-aminoquinoline-containing 2-imidazolines were synthesized via a one-pot 3-component condensation reaction of amine, aldehyde and…”
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Reversed Chloroquines Based on the 3,4-Dihydropyrimidin-2(1H)-one Scaffold: Synthesis and Evaluation for Antimalarial, b-Haematin Inhibition, and Cytotoxic Activity by October, Natasha, Watermeyer, Nicholas D, Yardley, Vanessa, Egan, Timothy J, Ncokazi, Kanyile, Chibale, Kelly

“…The synthesis, cytotoxicity, and antimalarial activity of resistance-reversing bifunctional dihydropyrimidone-chloroquinoline conjugates are reported herein…”
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