Kelso, Michael

Overview

The Kelso Research Group focuses on early stage antimicrobial and anticancer medicinal chemistry, drug discovery and chemical biology. We work with an extensive network of world leading local, national and international collaborators to explore the biological activities, both in vitro and in vivo, of innovative drug molecules designed and synthesised by the group at UOW.

Available as Research Supervisor

Selected Publications

Journal Article

Year	Title
2022	A novel and unexpected one pot synthesis of pyrrolo[1,2-a]quinolines Published In Tetrahedron Letters
2022	An amiloride derivative is active against the F1Fo-ATP synthase and cytochrome bd oxidase of Mycobacterium tuberculosis Published In Communications Biology
2022	Disruption of Water Networks is the Cause of Human/Mouse Species Selectivity in Urokinase Plasminogen Activator (uPA) Inhibitors Derived from Hexamethylene Amiloride (HMA) Published In Journal of Medicinal Chemistry
2022	Urokinase plasminogen activator as an anti-metastasis target: inhibitor design principles, recent amiloride derivatives, and issues with human/mouse species selectivity Published In Biophysical Reviews
2021	Novel amiloride derivatives that inhibit bacterial motility across multiple strains and stator types Published In Journal of Bacteriology
2021	Screening of 5- and 6-substituted amiloride libraries identifies dual-UPA/NHE1 active and single target-selective inhibitors Published In International Journal of Molecular Sciences
2021	Systematic evaluation of structure¿property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride Published In Bioorganic and Medicinal Chemistry
2020	6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease Published In Bioorganic and Medicinal Chemistry Letters
2020	Corrigendum to ¿Crystal structures and biochemical characterization of DNA sliding clamps from three Gram-negative bacterial pathogens¿ [J. Struct. Biol. 204 (3) (2018) 396¿405](S1047847718302818)(10.1016/j.jsb.2018.10.008) Published In Journal of Structural Biology
2020	Introduction of a Fixed-Charge, Photolabile Derivative for Enhanced Structural Elucidation of Fatty Acids Published In Analytical Chemistry
2020	Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study Published In Bioorganic and Medicinal Chemistry Letters
2020	The urokinase plasminogen activation system in rheumatoid arthritis: Pathophysiological roles and prospective therapeutic targets Published In Current Drug Targets
2020	Cephalosporin nitric oxide-donor prodrug DEA-C3D disperses biofilms formed by clinical cystic fibrosis isolates of Pseudomonas aeruginosa Published In Journal of Antimicrobial Chemotherapy
2020	Characterization of five novel anti-mrsa compounds identified using a whole-animal caenorhabditis elegans/galleria mellonella sequential-screening approach Published In Antibiotics
2020	Discovery of Cephalosporin-3'-Diazeniumdiolates That Show Dual Antibacterial and Antibiofilm Effects against Pseudomonas aeruginosa Clinical Cystic Fibrosis Isolates and Efficacy in a Murine Respiratory Infection Model Published In ACS Infectious Diseases
2020	Synthesis, structural/photophysical characterization and theoretical investigations with new β-pyridinium/quinolinium and β-bromine substituted bis(1,3-dimethylbarbituric acid) trimethine oxonol dyes that display large Stokes shifts Published In Dyes and Pigments
2019	6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease Published In Bioorganic and Medicinal Chemistry Letters
2019	Corrigendum to ¿Crystal structures and biochemical characterization of DNA sliding clamps from three Gram-negative bacterial pathogens¿ [J. Struct. Biol. 204 (3) (2018) 396¿405](S1047847718302818)(10.1016/j.jsb.2018.10.008) Published In Journal of Structural Biology
2019	Introduction of a Fixed-Charge, Photolabile Derivative for Enhanced Structural Elucidation of Fatty Acids Published In Analytical Chemistry
2019	Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study Published In Bioorganic and Medicinal Chemistry Letters
2019	The urokinase plasminogen activation system in rheumatoid arthritis: Pathophysiological roles and prospective therapeutic targets Published In Current Drug Targets
2018	6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer Published In Journal of Medicinal Chemistry
2018	Antibacterial Properties of Four Novel Hit Compounds from a Methicillin-Resistant Staphylococcus aureus-Caenorhabditis elegans High-Throughput Screen Published In Microbial Drug Resistance: mechanism, epidemiology, and disease
2018	Attaching NorA efflux pump inhibitors to methylene blue enhances antimicrobial photodynamic inactivation of Escherichia coli and Acinetobacter baumannii in vitro and in vivo Published In Bioorganic and Medicinal Chemistry Letters
2018	Crystal structures and biochemical characterization of DNA sliding clamps from three Gram-negative bacterial pathogens. Published In Journal of Structural Biology
2018	Mass spectrometry-directed structure elucidation and total synthesis of ultra-long chain (O-acyl)-ω-hydroxy fatty acids Published In Journal of Lipid Research
2018	Propyl-5-hydroxy-3-methyl-1-phenyl-1H-pyrazole-4-carbodithioate (HMPC): A new bacteriostatic agent against methicillin - Resistant Staphylococcus aureus Published In Scientific Reports
2018	Structure-activity relationships of pyrazole-4-carbodithioates as antibacterials against methicillin–resistant Staphylococcus aureus Published In Bioorganic and Medicinal Chemistry Letters
2017	89 Novel targeted nitric oxide donor pro-drugs disrupt biofilms formed by clinical Pseudomonas aeruginosa isolates from cystic fibrosis patients Published In Journal of Cystic Fibrosis
2017	Activity of a novel protonophore against methicillin-resistant Staphylococcus aureus Published In Future Medicinal Chemistry
2017	Attaching the NorA Efflux Pump Inhibitor INF55 to Methylene Blue Enhances Antimicrobial Photodynamic Inactivation of Methicillin-Resistant Staphylococcus aureus in Vitro and in Vivo Published In ACS Infectious Diseases
2017	Cephalosporin-3’ -diazeniumdiolate NO-donor prodrug PYRRO-C3D enhances azithromycin susceptibility of Non-typeable Haemophilus influenzae biofilms Published In Antimicrobial Agents and Chemotherapy
2017	Cephalosporin-NO-donor prodrug PYRRO-C3D shows β-lactam-mediated activity against Streptococcus pneumoniae biofilms Published In Nitric Oxide: Biology and Chemistry
2017	Low-Dose Nitric Oxide as Targeted Anti-biofilm Adjunctive Therapy to Treat Chronic Pseudomonas aeruginosa Infection in Cystic Fibrosis Published In Molecular Therapy
2017	Primary ciliary dyskinesia ciliated airway cells show increased susceptibility to Haemophilus influenzae biofilm formation Published In European Respiratory Journal
2017	Unexpected synthesis of 3-imino-2-(pyrrol-2-yl) isatogen derivatives affords facile access to a 2-pyrrolyl isatogen Published In Synthetic Communications: an international journal for rapid communication of synthetic organic chemistry
2016	5′-substituted amiloride derivatives as allosteric modulators binding in the sodium ion pocket of the adenosine A_2A receptor Published In Journal of Medicinal Chemistry
2016	Determination of ester position in isomeric (O-acyl)-hydroxy fatty acids by ion trap mass spectrometry Published In Rapid Communications in Mass Spectrometry
2016	Raf-kinase inhibitor GW5074 shows antibacterial activity against methicillin-resistant Staphylococcus aureus and potentiates the activity of gentamicin Published In Future Medicinal Chemistry
2016	Synthesis and preliminary evaluation of 5,7-dimethyl-2-aryl-3H-pyrrolizin-3-ones as angiogenesis inhibitors Published In Bioorganic and Medicinal Chemistry Letters
2015	Antibacterial properties of 3-(phenylsulfonyl)-2-pyrazinecarbonitrile Published In Bioorganic and Medicinal Chemistry Letters
2015	Bacterial sliding clamp inhibitors that mimic the sequential binding mechanism of endogenous linear motifs Published In Journal of Medicinal Chemistry
2015	Nitric oxide: a key mediator of biofilm dispersal with applications in infectious diseases Published In Current Pharmaceutical Design
2014	ChemInform Abstract: Synthesis, Structural Characterization, and Preliminary Evaluation of Non¿Indolin¿2¿one¿based Angiogenesis Inhibitors Related to Sunitinib (Sutent®). Published In ChemInform
2014	Clostridium difficile infection: molecular pathogenesis and novel therapeutics Published In Expert Review of Anti-infective Therapy
2014	DNA replication is the target for the antibacterial effects of nonsteroidal anti-inflammatory drugs Published In Chemistry and Biology
2014	Diarylacylhydrazones: Clostridium-selective antibacterials with activity against stationary-phase cells Published In Bioorganic and Medicinal Chemistry Letters
2014	Discovery of lead compounds targeting the bacterial sliding clamp using a fragment-based approach Published In Journal of Medicinal Chemistry
2014	Helical cyclic pentapeptides constrain HIV-1 Rev peptide for enhanced RNA binding Published In Tetrahedron: the international journal for the rapid publication of full original research papers and critical reviews in organic chemistr
2014	On the mechanism of berberine-INF55 (5-Nitro-2-phenylindole) hybrid antibacterials Published In Australian Journal of Chemistry: an international journal for chemical science
2014	RATNO - reducing antibiotic tolerance using nitric oxide in cystic fibrosis: report of a proof of concept clinical trial Published In Archives of Disease in Childhood
2013	A comparison of patient matched meibum and tear lipidomes Published In Investigative Ophthalmology and Visual Science
2013	Structural and thermodynamic dissection of linear motif recognition by the E. coli sliding clamp Published In Journal of Medicinal Chemistry
2013	Synthesis of cephalosporin-3′-diazeniumdiolates: biofilm dispersing NO-donor prodrugs activated by β-lactamase Published In Chemical Communications
2013	Synthesis, structural characterisation, and preliminary evaluation of non-indolin-2-one-based angiogenesis inhibitors related to sunitinib (Sutent®) Published In Australian Journal of Chemistry: an international journal for chemical science
2013	Synthesis, structural characterisation, and preliminary evaluation of non-indolin-2-one-based angiogenesis inhibitors related to sunitinib (SutentÃÂ®) Published In Australian Journal of Chemistry: an international journal for chemical science
2012	Cephalosporin-3'-diazeniumdiolates: Targeted NO-donor prodrugs for dispersing bacterial biofilms Published In Angewandte Chemie International Edition
2012	Cephalosporin¿3¿¿diazeniumdiolates: Targeted NO¿Donor Prodrugs for Dispersing Bacterial Biofilms Published In Angewandte Chemie
2012	ChemInform Abstract: Synthesis and Preliminary Evaluation of Amiloride Analogues as Inhibitors of the Urokinase¿Type Plasminogen Activator (uPA). Published In ChemInform
2012	Strategies to potentiate antimicrobial photoinactivation by overcoming resistant phenotypes Published In Photochemistry and Photobiology
2011	Anti-tumour/metastasis effects of the potassium-sparing diuretic amiloride: An orally active anti-cancer drug waiting for its call-of-duty? Published In International Journal of Cancer
2011	Small molecule antagonists of the urokinase (uPA): urokinase receptor (uPAR) interaction with high reported potencies show only weak effects in cell-based competition assays employing the native uPAR ligand Published In Bioorganic and Medicinal Chemistry
2011	Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA) Published In Bioorganic and Medicinal Chemistry Letters
2010	A mass spectrometric investigation of novel quadruplex DNA-selective berberine derivatives Published In Chemical Communications
2010	Berberine-INF55 (5-nitro-2-phenylindole) hybrid antimicrobials: effects of varying the relative orientation of the berberine and INF55 components Published In Antimicrobial Agents and Chemotherapy
2010	Synthesis of berberine-efflux pump inhibitor hybrid antibacterials Published In Synthetic Communications: an international journal for rapid communication of synthetic organic chemistry
2008	ChemInform Abstract: Oxidative Coupling of Indoles Using Thallium(III) Trifluoroacetate. Published In ChemInform
2008	ChemInform Abstract: Synthesis of an Anthracyclinone Bearing an Unprecedented Aromatic Ring¿Fused Bridgehead¿Hydroxylated Bicyclo[3.1.1]heptanol (I). Published In ChemInform
2008	Linkage Isomerism in the Binding of Pentapeptide Ac-His(Ala)(3)His-NH2 to (Ethylenediamine)Palladium(II): Effect of the Binding Mode on Peptide Conformation Published In Inorganic Chemistry: including bioinorganic chemistry
2008	Oxidative coupling of indoles using thallium(III) trifluoroacetate Published In Tetrahedron: the international journal for the rapid publication of full original research papers and critical reviews in organic chemistr
2008	Peptides and small molecules targeting the plasminogen activation system: Towards prophylactic anti-metastasis drugs for breast cancer Published In Recent Patents on Anti-Cancer Drug Discovery
2008	Structure-activity relationships of 2-aryl-1H-indole inhibitors of the NorA efflux pump in Staphylococcus aureus Published In Bioorganic and Medicinal Chemistry Letters
2007	Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase Published In Journal of Medicinal Chemistry
2007	Synthesis of an anthracyclinone bearing an unprecedented aromatic ring-fused bridgehead-hydroxylated bicyclo[3.1.1]heptanol Published In Tetrahedron Letters: the international journal for the rapid publication of all preliminary communications in organic chemistry
2004	Catalytic Enantioselective Conjugate Addition of Carbamates. Published In ChemInform
2003	A Cyclic Metallopeptide Induces ¿ Helicity in Short Peptide Fragments of Thermolysin Published In Angewandte Chemie
2001	Novel cylindrical, conical, and macrocyclic peptides from the cyclooligomerization of functionalized thiazole amino acids [2] Published In Journal of the American Chemical Society
2000	Anti-malarial effect of histone deacetylation inhibitors and mammalian tumour cytodifferentiating agents Published In International Journal for Parasitology
2000	The first solution stucture of a single ¿-helical turn. A pentapeptide ¿-helix stabilized by a metal clip [20] Published In Journal of the American Chemical Society
1999	Anti-tumour activity in vitro and in vivo of selective differentiating agents containing hydroxamate Published In British Journal of Cancer

Chapter

Year	Title
2010	Inhibitors of the Plasminogen Activation System - Promising New Agents for Suppressing Breat Cancer Metastasis Published In Frontiers in Anti-Cancer Drug Discovery
2002	Current approaches to peptidomimetics Published In Molecular Pathomechanisms and New Trends in Drug Research Publisher CRC Press

Conference Paper

Year	Title
2011	Synthesis and evaluation of dual-action hybrid antimicrobials and prodrugs Published In Abstracts of Papers of the American Chemical Society

Investigator On

Year	Title
2016 - 2020	Repurposing Amiloride Derivatives as New Agents for Drug-Resistant Tuberculosis Awarded by: Health Research Council of New Zealand (HRC) Funding Scheme: Grant
2016 - 2020	Repurposing Amiloride into Breast Cancer Drugs with a Dual-Targeting Mechanism Awarded by: National Health and Medical Research Council (NHMRC) Funding Scheme: Project Grant
2020	Organic & Medicinal Chemistry (OMC 2020) Conference Awarded by: NSW Government Department of Industry Funding Scheme: NSW Research Attraction and Acceleration Program
2018 - 2020	Molecular Interactions with an Antibiotic Target in DNA Replication Awarded by: Australian Research Council (ARC) Funding Scheme: Discovery Projects
2015 - 2018	Multi-Action antibiotics to treat chronic biofilm infections Awarded by: Cystic Fibrosis Australia (CFA) Funding Scheme: Research Grant
2014	Characterisation of tear film lipids Awarded by: Australian Research Council (ARC) Funding Scheme: Linkage Projects
2011 - 2014	Fragment-Based Screening Approaches for New Antibiotics Directed Against the Bacterial Sliding Clamp Awarded by: Australian Research Council (ARC) Funding Scheme: Discovery Projects
2011	Establishment of a comprehensive regional biophysical analysis facility Awarded by: Australian Research Council (ARC) Funding Scheme: Linkage Infrastructure Equipment & Facilities (LIEF)
2011	Investigation of novel adjunctive therapies to improve treatment success in paediatric middle ear infection (otitis media) Awarded by: Sparks - The Children's Medical Research Charity (UK) Funding Scheme: Sparks Innovation and Patient Benefit Grant (UK)
2010	Regional facility for molecular characterisation and mapping Awarded by: Australian Research Council (ARC) Funding Scheme: Linkage Infrastructure Equipment & Facilities (LIEF)
2009	The use of nitric oxide to control infections by biofilm forming bacteria Awarded by: National Health and Medical Research Council (NHMRC) Funding Scheme: Project Grant
2008	A synergy-based therapy against C.difficle Awarded by: National Institute of Health (NIH) Funding Scheme: Grant
	Antimicrobial Research Taskforce Awarded by: NUW Alliance Funding Scheme: Grant

Orcid Id

http://orcid.org/0000-0001-7809-6637 (confirmed)

Selected Publications

Journal Article

Year	Title
2022	A novel and unexpected one pot synthesis of pyrrolo[1,2-a]quinolines Published In Tetrahedron Letters
2022	An amiloride derivative is active against the F1Fo-ATP synthase and cytochrome bd oxidase of Mycobacterium tuberculosis Published In Communications Biology
2022	Disruption of Water Networks is the Cause of Human/Mouse Species Selectivity in Urokinase Plasminogen Activator (uPA) Inhibitors Derived from Hexamethylene Amiloride (HMA) Published In Journal of Medicinal Chemistry
2022	Urokinase plasminogen activator as an anti-metastasis target: inhibitor design principles, recent amiloride derivatives, and issues with human/mouse species selectivity Published In Biophysical Reviews
2021	Novel amiloride derivatives that inhibit bacterial motility across multiple strains and stator types Published In Journal of Bacteriology
2021	Screening of 5- and 6-substituted amiloride libraries identifies dual-UPA/NHE1 active and single target-selective inhibitors Published In International Journal of Molecular Sciences
2021	Systematic evaluation of structure¿property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride Published In Bioorganic and Medicinal Chemistry
2020	6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease Published In Bioorganic and Medicinal Chemistry Letters
2020	Corrigendum to ¿Crystal structures and biochemical characterization of DNA sliding clamps from three Gram-negative bacterial pathogens¿ [J. Struct. Biol. 204 (3) (2018) 396¿405](S1047847718302818)(10.1016/j.jsb.2018.10.008) Published In Journal of Structural Biology
2020	Introduction of a Fixed-Charge, Photolabile Derivative for Enhanced Structural Elucidation of Fatty Acids Published In Analytical Chemistry
2020	Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study Published In Bioorganic and Medicinal Chemistry Letters
2020	The urokinase plasminogen activation system in rheumatoid arthritis: Pathophysiological roles and prospective therapeutic targets Published In Current Drug Targets
2020	Cephalosporin nitric oxide-donor prodrug DEA-C3D disperses biofilms formed by clinical cystic fibrosis isolates of Pseudomonas aeruginosa Published In Journal of Antimicrobial Chemotherapy
2020	Characterization of five novel anti-mrsa compounds identified using a whole-animal caenorhabditis elegans/galleria mellonella sequential-screening approach Published In Antibiotics
2020	Discovery of Cephalosporin-3'-Diazeniumdiolates That Show Dual Antibacterial and Antibiofilm Effects against Pseudomonas aeruginosa Clinical Cystic Fibrosis Isolates and Efficacy in a Murine Respiratory Infection Model Published In ACS Infectious Diseases
2020	Synthesis, structural/photophysical characterization and theoretical investigations with new β-pyridinium/quinolinium and β-bromine substituted bis(1,3-dimethylbarbituric acid) trimethine oxonol dyes that display large Stokes shifts Published In Dyes and Pigments
2019	6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease Published In Bioorganic and Medicinal Chemistry Letters
2019	Corrigendum to ¿Crystal structures and biochemical characterization of DNA sliding clamps from three Gram-negative bacterial pathogens¿ [J. Struct. Biol. 204 (3) (2018) 396¿405](S1047847718302818)(10.1016/j.jsb.2018.10.008) Published In Journal of Structural Biology
2019	Introduction of a Fixed-Charge, Photolabile Derivative for Enhanced Structural Elucidation of Fatty Acids Published In Analytical Chemistry
2019	Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study Published In Bioorganic and Medicinal Chemistry Letters
2019	The urokinase plasminogen activation system in rheumatoid arthritis: Pathophysiological roles and prospective therapeutic targets Published In Current Drug Targets
2018	6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer Published In Journal of Medicinal Chemistry
2018	Antibacterial Properties of Four Novel Hit Compounds from a Methicillin-Resistant Staphylococcus aureus-Caenorhabditis elegans High-Throughput Screen Published In Microbial Drug Resistance: mechanism, epidemiology, and disease
2018	Attaching NorA efflux pump inhibitors to methylene blue enhances antimicrobial photodynamic inactivation of Escherichia coli and Acinetobacter baumannii in vitro and in vivo Published In Bioorganic and Medicinal Chemistry Letters
2018	Crystal structures and biochemical characterization of DNA sliding clamps from three Gram-negative bacterial pathogens. Published In Journal of Structural Biology
2018	Mass spectrometry-directed structure elucidation and total synthesis of ultra-long chain (O-acyl)-ω-hydroxy fatty acids Published In Journal of Lipid Research
2018	Propyl-5-hydroxy-3-methyl-1-phenyl-1H-pyrazole-4-carbodithioate (HMPC): A new bacteriostatic agent against methicillin - Resistant Staphylococcus aureus Published In Scientific Reports
2018	Structure-activity relationships of pyrazole-4-carbodithioates as antibacterials against methicillin–resistant Staphylococcus aureus Published In Bioorganic and Medicinal Chemistry Letters
2017	89 Novel targeted nitric oxide donor pro-drugs disrupt biofilms formed by clinical Pseudomonas aeruginosa isolates from cystic fibrosis patients Published In Journal of Cystic Fibrosis
2017	Activity of a novel protonophore against methicillin-resistant Staphylococcus aureus Published In Future Medicinal Chemistry
2017	Attaching the NorA Efflux Pump Inhibitor INF55 to Methylene Blue Enhances Antimicrobial Photodynamic Inactivation of Methicillin-Resistant Staphylococcus aureus in Vitro and in Vivo Published In ACS Infectious Diseases
2017	Cephalosporin-3’ -diazeniumdiolate NO-donor prodrug PYRRO-C3D enhances azithromycin susceptibility of Non-typeable Haemophilus influenzae biofilms Published In Antimicrobial Agents and Chemotherapy
2017	Cephalosporin-NO-donor prodrug PYRRO-C3D shows β-lactam-mediated activity against Streptococcus pneumoniae biofilms Published In Nitric Oxide: Biology and Chemistry
2017	Low-Dose Nitric Oxide as Targeted Anti-biofilm Adjunctive Therapy to Treat Chronic Pseudomonas aeruginosa Infection in Cystic Fibrosis Published In Molecular Therapy
2017	Primary ciliary dyskinesia ciliated airway cells show increased susceptibility to Haemophilus influenzae biofilm formation Published In European Respiratory Journal
2017	Unexpected synthesis of 3-imino-2-(pyrrol-2-yl) isatogen derivatives affords facile access to a 2-pyrrolyl isatogen Published In Synthetic Communications: an international journal for rapid communication of synthetic organic chemistry
2016	5′-substituted amiloride derivatives as allosteric modulators binding in the sodium ion pocket of the adenosine A_2A receptor Published In Journal of Medicinal Chemistry
2016	Determination of ester position in isomeric (O-acyl)-hydroxy fatty acids by ion trap mass spectrometry Published In Rapid Communications in Mass Spectrometry
2016	Raf-kinase inhibitor GW5074 shows antibacterial activity against methicillin-resistant Staphylococcus aureus and potentiates the activity of gentamicin Published In Future Medicinal Chemistry
2016	Synthesis and preliminary evaluation of 5,7-dimethyl-2-aryl-3H-pyrrolizin-3-ones as angiogenesis inhibitors Published In Bioorganic and Medicinal Chemistry Letters
2015	Antibacterial properties of 3-(phenylsulfonyl)-2-pyrazinecarbonitrile Published In Bioorganic and Medicinal Chemistry Letters
2015	Bacterial sliding clamp inhibitors that mimic the sequential binding mechanism of endogenous linear motifs Published In Journal of Medicinal Chemistry
2015	Nitric oxide: a key mediator of biofilm dispersal with applications in infectious diseases Published In Current Pharmaceutical Design
2014	ChemInform Abstract: Synthesis, Structural Characterization, and Preliminary Evaluation of Non¿Indolin¿2¿one¿based Angiogenesis Inhibitors Related to Sunitinib (Sutent®). Published In ChemInform
2014	Clostridium difficile infection: molecular pathogenesis and novel therapeutics Published In Expert Review of Anti-infective Therapy
2014	DNA replication is the target for the antibacterial effects of nonsteroidal anti-inflammatory drugs Published In Chemistry and Biology
2014	Diarylacylhydrazones: Clostridium-selective antibacterials with activity against stationary-phase cells Published In Bioorganic and Medicinal Chemistry Letters
2014	Discovery of lead compounds targeting the bacterial sliding clamp using a fragment-based approach Published In Journal of Medicinal Chemistry
2014	Helical cyclic pentapeptides constrain HIV-1 Rev peptide for enhanced RNA binding Published In Tetrahedron: the international journal for the rapid publication of full original research papers and critical reviews in organic chemistr
2014	On the mechanism of berberine-INF55 (5-Nitro-2-phenylindole) hybrid antibacterials Published In Australian Journal of Chemistry: an international journal for chemical science
2014	RATNO - reducing antibiotic tolerance using nitric oxide in cystic fibrosis: report of a proof of concept clinical trial Published In Archives of Disease in Childhood
2013	A comparison of patient matched meibum and tear lipidomes Published In Investigative Ophthalmology and Visual Science
2013	Structural and thermodynamic dissection of linear motif recognition by the E. coli sliding clamp Published In Journal of Medicinal Chemistry
2013	Synthesis of cephalosporin-3′-diazeniumdiolates: biofilm dispersing NO-donor prodrugs activated by β-lactamase Published In Chemical Communications
2013	Synthesis, structural characterisation, and preliminary evaluation of non-indolin-2-one-based angiogenesis inhibitors related to sunitinib (Sutent®) Published In Australian Journal of Chemistry: an international journal for chemical science
2013	Synthesis, structural characterisation, and preliminary evaluation of non-indolin-2-one-based angiogenesis inhibitors related to sunitinib (SutentÃÂ®) Published In Australian Journal of Chemistry: an international journal for chemical science
2012	Cephalosporin-3'-diazeniumdiolates: Targeted NO-donor prodrugs for dispersing bacterial biofilms Published In Angewandte Chemie International Edition
2012	Cephalosporin¿3¿¿diazeniumdiolates: Targeted NO¿Donor Prodrugs for Dispersing Bacterial Biofilms Published In Angewandte Chemie
2012	ChemInform Abstract: Synthesis and Preliminary Evaluation of Amiloride Analogues as Inhibitors of the Urokinase¿Type Plasminogen Activator (uPA). Published In ChemInform
2012	Strategies to potentiate antimicrobial photoinactivation by overcoming resistant phenotypes Published In Photochemistry and Photobiology
2011	Anti-tumour/metastasis effects of the potassium-sparing diuretic amiloride: An orally active anti-cancer drug waiting for its call-of-duty? Published In International Journal of Cancer
2011	Small molecule antagonists of the urokinase (uPA): urokinase receptor (uPAR) interaction with high reported potencies show only weak effects in cell-based competition assays employing the native uPAR ligand Published In Bioorganic and Medicinal Chemistry
2011	Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA) Published In Bioorganic and Medicinal Chemistry Letters
2010	A mass spectrometric investigation of novel quadruplex DNA-selective berberine derivatives Published In Chemical Communications
2010	Berberine-INF55 (5-nitro-2-phenylindole) hybrid antimicrobials: effects of varying the relative orientation of the berberine and INF55 components Published In Antimicrobial Agents and Chemotherapy
2010	Synthesis of berberine-efflux pump inhibitor hybrid antibacterials Published In Synthetic Communications: an international journal for rapid communication of synthetic organic chemistry
2008	ChemInform Abstract: Oxidative Coupling of Indoles Using Thallium(III) Trifluoroacetate. Published In ChemInform
2008	ChemInform Abstract: Synthesis of an Anthracyclinone Bearing an Unprecedented Aromatic Ring¿Fused Bridgehead¿Hydroxylated Bicyclo[3.1.1]heptanol (I). Published In ChemInform
2008	Linkage Isomerism in the Binding of Pentapeptide Ac-His(Ala)(3)His-NH2 to (Ethylenediamine)Palladium(II): Effect of the Binding Mode on Peptide Conformation Published In Inorganic Chemistry: including bioinorganic chemistry
2008	Oxidative coupling of indoles using thallium(III) trifluoroacetate Published In Tetrahedron: the international journal for the rapid publication of full original research papers and critical reviews in organic chemistr
2008	Peptides and small molecules targeting the plasminogen activation system: Towards prophylactic anti-metastasis drugs for breast cancer Published In Recent Patents on Anti-Cancer Drug Discovery
2008	Structure-activity relationships of 2-aryl-1H-indole inhibitors of the NorA efflux pump in Staphylococcus aureus Published In Bioorganic and Medicinal Chemistry Letters
2007	Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase Published In Journal of Medicinal Chemistry
2007	Synthesis of an anthracyclinone bearing an unprecedented aromatic ring-fused bridgehead-hydroxylated bicyclo[3.1.1]heptanol Published In Tetrahedron Letters: the international journal for the rapid publication of all preliminary communications in organic chemistry
2004	Catalytic Enantioselective Conjugate Addition of Carbamates. Published In ChemInform
2003	A Cyclic Metallopeptide Induces ¿ Helicity in Short Peptide Fragments of Thermolysin Published In Angewandte Chemie
2001	Novel cylindrical, conical, and macrocyclic peptides from the cyclooligomerization of functionalized thiazole amino acids [2] Published In Journal of the American Chemical Society
2000	Anti-malarial effect of histone deacetylation inhibitors and mammalian tumour cytodifferentiating agents Published In International Journal for Parasitology
2000	The first solution stucture of a single ¿-helical turn. A pentapeptide ¿-helix stabilized by a metal clip [20] Published In Journal of the American Chemical Society
1999	Anti-tumour activity in vitro and in vivo of selective differentiating agents containing hydroxamate Published In British Journal of Cancer

Chapter

Year	Title
2010	Inhibitors of the Plasminogen Activation System - Promising New Agents for Suppressing Breat Cancer Metastasis Published In Frontiers in Anti-Cancer Drug Discovery
2002	Current approaches to peptidomimetics Published In Molecular Pathomechanisms and New Trends in Drug Research Publisher CRC Press

Conference Paper

Year	Title
2011	Synthesis and evaluation of dual-action hybrid antimicrobials and prodrugs Published In Abstracts of Papers of the American Chemical Society

Investigator On

Year	Title
2016 - 2020	Repurposing Amiloride Derivatives as New Agents for Drug-Resistant Tuberculosis Awarded by: Health Research Council of New Zealand (HRC) Funding Scheme: Grant
2016 - 2020	Repurposing Amiloride into Breast Cancer Drugs with a Dual-Targeting Mechanism Awarded by: National Health and Medical Research Council (NHMRC) Funding Scheme: Project Grant
2020	Organic & Medicinal Chemistry (OMC 2020) Conference Awarded by: NSW Government Department of Industry Funding Scheme: NSW Research Attraction and Acceleration Program
2018 - 2020	Molecular Interactions with an Antibiotic Target in DNA Replication Awarded by: Australian Research Council (ARC) Funding Scheme: Discovery Projects
2015 - 2018	Multi-Action antibiotics to treat chronic biofilm infections Awarded by: Cystic Fibrosis Australia (CFA) Funding Scheme: Research Grant
2014	Characterisation of tear film lipids Awarded by: Australian Research Council (ARC) Funding Scheme: Linkage Projects
2011 - 2014	Fragment-Based Screening Approaches for New Antibiotics Directed Against the Bacterial Sliding Clamp Awarded by: Australian Research Council (ARC) Funding Scheme: Discovery Projects
2011	Establishment of a comprehensive regional biophysical analysis facility Awarded by: Australian Research Council (ARC) Funding Scheme: Linkage Infrastructure Equipment & Facilities (LIEF)
2011	Investigation of novel adjunctive therapies to improve treatment success in paediatric middle ear infection (otitis media) Awarded by: Sparks - The Children's Medical Research Charity (UK) Funding Scheme: Sparks Innovation and Patient Benefit Grant (UK)
2010	Regional facility for molecular characterisation and mapping Awarded by: Australian Research Council (ARC) Funding Scheme: Linkage Infrastructure Equipment & Facilities (LIEF)
2009	The use of nitric oxide to control infections by biofilm forming bacteria Awarded by: National Health and Medical Research Council (NHMRC) Funding Scheme: Project Grant
2008	A synergy-based therapy against C.difficle Awarded by: National Institute of Health (NIH) Funding Scheme: Grant
	Antimicrobial Research Taskforce Awarded by: NUW Alliance Funding Scheme: Grant

Orcid Id

http://orcid.org/0000-0001-7809-6637 (confirmed)

Kelso, Michael Professor

Professor

Overview

Overview

Available as Research Supervisor

Publications

Selected Publications

Journal Article

Chapter

Conference Paper

Funding

Investigator On

Identity

Orcid Id

Overview

Publications

Selected Publications

Journal Article

Chapter

Conference Paper

Funding

Investigator On

Identity

Orcid Id

Visualisations