A5067495747- Dendrimers and Hyperbranched Polymers
- Ferrocene Chemistry and Applications
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Metal complexes synthesis and properties
- Crystallography and molecular interactions
- Cancer therapeutics and mechanisms
- Chemical Synthesis and Analysis
- RNA Interference and Gene Delivery
- Tuberculosis Research and Epidemiology
- Synthesis and biological activity
- Organometallic Complex Synthesis and Catalysis
- Organometallic Compounds Synthesis and Characterization
- Magnetism in coordination complexes
- Synthesis and Biological Evaluation
- Covalent Organic Framework Applications
- Advanced Photocatalysis Techniques
- Pharmacogenetics and Drug Metabolism
- Bioactive Compounds and Antitumor Agents
- Synthesis of Tetrazole Derivatives
- Drug Transport and Resistance Mechanisms
- Advanced biosensing and bioanalysis techniques
- Computational Drug Discovery Methods
- HIV/AIDS drug development and treatment
- Metabolism and Genetic Disorders
University of Cape Town
2009-2025
City of Cape Town
2016
Chelating neutral (N,O) and cationic (N,N) first- second-generation ruthenium(II) arene metallodendrimers based on poly(propyleneimine) dendrimer scaffolds were obtained from dinuclear ruthenium precursors by reactions with salicylaldimine iminopyridyl dendritic ligands, respectively. The N,N complexes isolated as hexafluorophosphate salts characterised NMR IR spectroscopy, MALDI-TOF mass spectrometry. Related mononuclear in a similar manner their molecular structures have been determined...
The first CO-releasing metallodendrimers, based on polypyridyl dendritic scaffolds functionalized with Mn(CO)3 moieties, of the general formula [DAB-PPI-{MnBr(bpyCH3,CH═N)(CO)3}n], where DAB = 1,4-diaminobutane, PPI poly(propyleneimine), bpy bipyridyl, and n 4 for first- or 8 second-generation dendrimers, were synthesized comprehensively characterized by analytical (HR-ESI mass spectrometry elemental analysis) spectroscopic (1H, 13C{1H}-NMR, infrared, UV/vis spectroscopy) methods. CO-release...
Abstract The field of biomedical metallodendrimers is an emerging discipline that attracting prolific attention. Metallodendrimers, like their organic counterparts, are known for multivalency (high concentration peripheral end‐groups), well‐defined architectures and narrow polydispersity. These characteristics make well‐suited as innovative scaffolds the development new therapeutic agents. Coupled with surge interest in use various metal complexes to treat diseases, application medicinal...
Cationic N,O-chelating dendrimers functionalised on the periphery with RAPTA-like (ruthenium(II)-arene-1,3,5-triaza-7-phosphatricyclo[3.3.1.1]decane) moieties have been synthesised and characterised using NMR IR spectroscopy, elemental analysis MALDI-TOF/HR-ESI mass spectrometry. Metallodendrimers from first to fourth-generation containing up 32 peripheral ruthenium-arene-PTA were obtained. Model mononuclear analogues, [{Ru(η(6)-p-cymene)((C(7)H(5)NO)-κ(2)-N,O)(PTA)}((CH(2))(3))][PF(6)]...
Thirteen new ruthenium and osmium half-sandwich complexes with chloroquine analogue ligands have been synthesized evaluated for anti-malarial properties.
New antibiotics with either a novel mode of action or inhibition are urgently needed to overcome the threat drug-resistant tuberculosis (TB). The present study profiles new spiropyrimidinetriones (SPTs), DNA gyrase inhibitors having activity against Mycobacterium (Mtb), causative agent TB. While clinical candidate zoliflodacin has progressed phase 3 trials for treatment gonorrhea, compounds herein demonstrated higher inhibitory potency Mtb (e.g., compound 42 IC50 = 2.0) and lower minimum...
A new series of eight first- and second-generation heterometallic ferrocenyl-derived metal-arene metallodendrimers, containing ruthenium(ii)-p-cymene, ruthenium(ii)-hexamethylbenzene, rhodium(iii)-cyclopentadienyl or iridium(iii)-cyclopentadienyl moieties have been prepared. The metallodendrimers were synthesized by first reacting DAB-(NH2)n (where n = 4 8, DAB diaminobutane) with salicylaldehyde, then the Schiff-base dendritic ligands reacted in a one-pot reaction appropriate...
Mefloquine is an antimalarial drug routinely used for prophylaxis and in the treatment of malaria. Approximately 50% mefloquine metabolism, both vitro vivo, mediated by CYP3A4 with remaining contributions other CYP450 isoforms unaccounted for. This study aimed to determine contribution CYP450s metabolism incorporate this knowledge into a physiologically-based pharmacokinetic model. The data human liver microsomes demonstrated involvement CYP3A4/5 as well previously unreported CYP1A2...
Four first- and second-generation heterometallic ferrocenyl derived p-cymene-Ru(II) metallodendrimers, of general formula [DAB-PPI{(η6-p-cymene)Ru((C7H5NO)-κ2-N,O)PTA(5-ferrocenylvinyl)}n][PF6]n [DAB-PPI{(η6-p-cymene)Ru((C6H5N2)-κ2-N,N)Cl(5-ferrocenylvinyl)}n][PF6]n (where n = 4 (G1), 8 (G2), DAB 1,4-diaminobutane, PPI poly(propyleneimine), PTA 1,3,5-triaza-7-phosphatricyclo[3.3.1.1]decane) have been synthesized. All complexes characterized using analytical (i.e., HR-ESI mass spectrometry,...
Described here is a series of spiropyrimidinetrione (SPT) compounds with activity against Mycobacterium tuberculosis through inhibition DNA gyrase. The SPT class operates via novel mode inhibition, which involves Mg 2+ -independent stabilization the cleavage complex gyrase and thereby not cross-resistant other gyrase-inhibiting antibacterials, including fluoroquinolones.
Abstract Dendrimers of different generations and core structures [diaminobutane poly(propylenimine) (DAB) G1, G2, G3; poly(amidoamine) (PAMAM) G1] were chosen as carriers for bioactive organometallic half‐sandwich complexes the type CpM(CO) 3 (Cp = cyclopentadienyl, M Mn or Re) to study influence these parameters on their biological activity against cancer cells. Structure–activity relationships determined by variation metal center well type, molecular weight, number terminal functional...
Tricarbonylrhenium(I) metallodendrimers functionalized with N , ‐2‐picolylamino chelates have been synthesized by the [2+1] approach. Methanol substitution reactions of first‐ and second‐generation poly(propylene amine) tetra‐ octanuclear rhenium a range monodentate nucleophiles (i.e. 4‐dimethylaminopyridine, pyridine, bromide ions) were investigated compared to an analogous monomeric complex, fac ‐[Re(CO) 3 ( ‐bidentate)(CH OH)] + . These detailed kinetic studies reveal that greater...