Research Topics
| J B BremnerSummaryAffiliation: University of Wollongong Country: Australia Publications
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Detail Information
Publications
In vitro cytotoxicity evaluation of some substituted isatin derivativesKara L Vine
School of Biological Sciences, University of Wollongong, NSW 2522, Australia
Bioorg Med Chem 15:931-8. 2007..These results indicate that di- and tri-substituted isatins may be useful leads for anticancer drug development in the future...- An investigation into the cytotoxicity and mode of action of some novel N-alkyl-substituted isatinsKara L Vine
School of Biological Sciences, and Department of Chemistry, University of Wollongong, NSW 2522, Australia
J Med Chem 50:5109-17. 2007..49 muM. Various N-alkylisatins were also found to dramatically alter lymphocyte morphology, destabilize microtubules, inhibit tubulin polymerization, induce G2/M cell cycle arrest, and activate the effector caspase-3 and -7... 
Synthesis and structural characterization of 1-[2-(5-nitro-1H-indol-2-yl)phenyl]methylpyridinium chlorideJohn B Bremner
School of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia
Molecules 16:7627-33. 2011..u.) = 4; R1 = 0.048, and wR2 = 0.13. Of interest in the single crystal X-ray structure is the (intramolecular) disposition of the pyridinium plane over the indole heterocyclic residue [interplanar dihedral angle 17.91(4)°]...- Dual action-based approaches to antibacterial agentsJohn B Bremner
Department of Chemistry, University of Wollongong, Wollongong, NSW, 2522, Australia
Curr Med Chem 14:1459-77. 2007..In particular the areas reviewed include the use of two drugs in combination, dual action prodrugs, and dual action drugs (or hybrid drugs)... - Synthesis and nicotinic receptor activity of a hydroxylated tropaneJohn B Bremner
Department of Chemistry and Institute for Biomolecular Science, University of Wollongong, Wollongong, NSW 2522, Australia
Bioorg Med Chem Lett 14:271-3. 2004..Compound 4 also displayed generally similar binding and selectivity profiles at alpha(4)beta(2), alpha(2)beta(4), alpha(3)beta(4), and alpha(4)beta(4) nAChR subtypes to those for nicotine... - Ligand design for alpha(1) adrenoceptorsJ B Bremner
Department of Chemistry, University of Wollongong, Wollongong, NSW, 2522, Australia
Curr Med Chem 8:607-20. 2001..A new combined approach using pharmacophores and receptor docking affords possibilities for deeper insights into achieving small molecule binding selectivity... - Ligand design for alpha1 adrenoceptor subtype selective antagonistsJ B Bremner
Department of Chemistry, University of Wollongong, NSW, Australia
Bioorg Med Chem 8:201-14. 2000..The first preliminary antagonist pharmacophore model for the alpha1D adrenoceptor subtype is also reported... - Chemical defense in the egg masses of benthic invertebrates: an assessment of antibacterial activity in 39 mollusks and 4 polychaetesK Benkendorff
Department of Biological Sciences, University of Wollongong, New South Wales, 2522, Australia
J Invertebr Pathol 78:109-18. 2001..The results of this study indicate that a wide range of invertebrates use chemical defense to protect their early stage embryos against bacterial infection... - Synthesis and antibacterial studies of binaphthyl-based tripeptoids. Part 1John B Bremner
School of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia
Bioorg Med Chem 18:2611-20. 2010..9-3.9microg/mL against Staphylococcus aureus. One peptoid had a MIC value of 6microg/mL against a methicillin-resistant strain of S. aureus (MRSA) and a MIC value of 2microg/mL against vancomycin-resistant strains of enterococci (VRE)... - N-phenethyl and N-naphthylmethyl isatins and analogues as in vitro cytotoxic agentsLidia Matesic
School of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia
Bioorg Med Chem 16:3118-24. 2008..The results allowed further development of structure-activity relationships. The compound 5,7-dibromo-N-(1-naphthylmethyl)-1H-indole-2,3-dione 5a was the most potent against U937 cells with an IC(50) value of 0.19 microM... - Synthesis and biological evaluation of bicyclic and tricyclic substituted nortropane derivatives: discovery of a novel selective alpha1D-adrenergic receptor ligandSusan J McGinty
Institute for Biomolecular Science and Department of Chemistry, University of Wollongong, Northfields Ave, Wollongong, NSW 2522, Australia
Bioorg Med Chem 12:5639-50. 2004..2.1]octan-3-spiro-2'-(1',3'-dioxolane)-6-ol, a novel lead compound selective for the alpha(1D)-adrenergic receptor, is reported... 
Berberine-INF55 (5-nitro-2-phenylindole) hybrid antimicrobials: effects of varying the relative orientation of the berberine and INF55 componentsDanuta Tomkiewicz
School of Chemistry, University of Wollongong, Northfields Ave, NSW 2522, Australia
Antimicrob Agents Chemother 54:3219-24. 2010..In summary, subtle repositioning of the pump-blocking INF55 moiety in berberine-INF55 hybrids was found to have a minimal effect on their antibacterial activities but to significantly alter their effects on MDR pumps...- Synthesis of functionalized 2-aryl-5-nitro-1H-indoles and their activity as bacterial NorA efflux pump inhibitorsSiritron Samosorn
Institute for Biomolecular Science, Department of Chemistry, University of Wollongong, NSW 2522, Australia
Bioorg Med Chem 14:857-65. 2006..The compound [4-benzyloxy-2-(5-nitro-1H-2-yl)-phenyl]-methanol was the most potent pump inhibitor... - Structure-activity relationships of 2-aryl-1H-indole inhibitors of the NorA efflux pump in Staphylococcus aureusJoseph I Ambrus
School of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia
Bioorg Med Chem Lett 18:4294-7. 2008..A promising new antibacterial lead compound against S. aureus (2-phenyl-1H-indol-5-yl)-methanol, was also found... - Synthesis of novel N-protected hydrophobic phenylalanines and their application in potential antibacterialsTimothy P Boyle
School of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia
Eur J Med Chem 44:1001-9. 2009..An efficient synthesis of two new N-acetyl-4'-arylphenylalanines is described together with their incorporation into a number of cationic peptoid antibacterial agents, one of which had an MIC of 7.8 microg/mL against Staphylococcus aureus... - Modelling of adrenoceptor ligand targets based on novel medium- or macro-sized fused nitrogen heterocyclic systemsR Griffith
Department of Chemistry, University of Wollongong, NSW, Australia
J Comput Aided Mol Des 13:69-78. 1999..None of the potential targets were closely enough related in this case to the lead compound to warrant synthesis... - Mining the Chemical Abstracts database with pharmacophore-based queriesJohn B Bremner
Department of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia
J Mol Graph Model 21:185-94. 2002..Several structurally novel rigid ring skeletons were found with this new database mining technique which are potentially useful as leads in the design of alpha1B selective adrenergic receptor antagonists... - Binaphthyl scaffolded peptoids via ring-closing metathesis reactions and their anti-bacterial activitiesAdel Garas
School of Chemistry, University of Wollongong, Wollongong, NSW, Australia
Bioorg Med Chem Lett 19:3010-3. 2009..An efficient synthesis of four new acyclic and four new cyclic binaphthyl-based cationic peptoids is described. These compounds had anti-bacterial activities with MIC values of 4-62 microg/mL against Staphylococcus aureus... - Isolation and NMR spectroscopic clarification of the alkaloid 1,3,7-trimethylguanine from the ascidian Eudistoma maculosumY Berry
Department of Chemistry, University of Wollongong, Wollongong, NSW 2522, Australia
Nat Prod Res 20:479-83. 2006..The alkaloid 1,3,7-trimethylguanine was isolated from the ascidian Eudistoma maculosum, and differences in the NMR spectroscopic data for this compound compared with data in the literature are due to ammonium salt formation... - Development and assessment of novel all-in-one parenteral formulations with integrated anticoagulant properties for the concomitant delivery of 5-fluorouracil and calcium folinateJulie M Locke
School of Chemistry, University of Wollongong, Wollongong, New South Wales, Australia
Anticancer Drugs 20:822-31. 2009.... - 2,4,5-Tribromo-1H-imidazole in the egg masses of three muricid molluscsKirsten Benkendorff
Department of Chemistry and Institute for Biomolecular Science, University of Wollongong, NSW, Australia, 2522
Nat Prod Res 18:427-31. 2004..This imidazole is likely to be responsible for some of the antimicrobial activity observed in the egg extracts. This is the first report of this compound from a natural source... - Selective targeting of 2'-deoxy-5-fluorouridine to urokinase positive malignant cells in vitroKara L Vine
School of Biological Sciences and Centre for Medical Bioscience, University of Wollongong, NSW 2522, Australia v
Bioorg Med Chem Lett 20:2908-11. 2010..Up to 7 molecules of 5-FUdr were incorporated per PAI-2 molecule without affecting protein activity. This is the first time a small organic cytotoxin has been conjugated to PAI-2... - Selectivity of an indolyl berberine derivative for tetrameric G-quadruplex DNAKarina C Gornall
Department of Chemistry, University of Wollongong, NSW 2522, Australia
Rapid Commun Mass Spectrom 21:1759-66. 2007..These investigations show that SS14 is a promising lead compound for drugs that may selectively bind quadruplex over duplex DNA... - Antiplasmodial activity of atisinium chloride from the Bhutanese medicinal plant, Aconitum orochryseumPhurpa Wangchuk
School of Chemistry, University of Wollongong, Wollongong, NSW, Australia
J Ethnopharmacol 130:559-62. 2010..The plant Aconitum orochryseum Stapf. (Ranunculaceae) is employed together with other plants in Bhutanese traditional medicine and is indicated for malaria-associated fever...