All Stories

  1. Advances in Anthelmintic Target Identification

    Article • International Journal of Molecular Sciences, April 2025, MDPI AG

    Dr Brad E Sleebs

  2. Optimization and Characterization of N-Acetamide Indoles as Antimalarials That Target PfATP4

    Article • Journal of Medicinal Chemistry, April 2025, American Chemical Society (ACS)

    Dr Brad E Sleebs

  3. Prediction and Prioritisation of Novel Anthelmintic Candidates from Public Databases Using Deep Learning and Available Bioactivity Data Sets

    Article • International Journal of Molecular Sciences, March 2025, MDPI AG

    Dr Brad E Sleebs

  4. Structure–activity analysis of imino‐pyrimidinone‐fused pyrrolidines aids the development of dual plasmepsin V and plasmepsin X inhibitors

    Article • European Journal of Biochemistry, March 2025, Wiley

    Dr Brad E Sleebs

  5. Exploration and characterization of the antimalarial activity of cyclopropyl carboxamides that target the mitochondrial protein, cytochrome b

    Article • European Journal of Medicinal Chemistry, December 2024, Elsevier

    Dr Brad E Sleebs

  6. Lactam Truncation Yields a Dihydroquinazolinone Scaffold with Potent Antimalarial Activity that Targets PfATP4

    Article • ChemMedChem, October 2024, Wiley

    Dr Brad E Sleebs

  7. An adaptable, fit-for-purpose screening approach with high-throughput capability to determine speed of action and stage specificity of anti-malarial compounds

    Article • Antimicrobial Agents and Chemotherapy, October 2024, ASM Journals

    Dr Brad E Sleebs

  8. Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3

    Article • European Journal of Medicinal Chemistry, October 2024, Elsevier

    Dr Brad E Sleebs

  9. Property and Activity Refinement of Dihydroquinazolinone-3-carboxamides as Orally Efficacious Antimalarials that Target PfATP4

    Article • Journal of Medicinal Chemistry, August 2024, American Chemical Society (ACS)

    Dr Brad E Sleebs

  10. Comparative structure activity and target exploration of 1,2-diphenylethynes in Haemonchus contortus and Caenorhabditis elegans

    Article • International Journal for Parasitology Drugs and Drug Resistance, August 2024, Elsevier

    Dr Brad E Sleebs

  11. Aryl amino acetamides prevent Plasmodium falciparum ring development via targeting the lipid-transfer protein PfSTART1

    Article • Nature Communications, June 2024, Springer Science + Business Media

    Dr Brad E Sleebs

  12. Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein

    Article • European Journal of Medicinal Chemistry, April 2024, Elsevier

    Dr Brad E Sleebs

  13. Structure-activity relationship and target investigation of 2-aryl quinolines with nematocidal activity

    Article • International Journal for Parasitology Drugs and Drug Resistance, April 2024, Elsevier

    Dr Brad E Sleebs

  14. A phenotypic screen of the Global Health Priority Box identifies an insecticide with anthelmintic activity

    Article • Parasites & Vectors, March 2024, Springer Science + Business Media

    Dr Brad E Sleebs

  15. BNC210, a negative allosteric modulator of the alpha 7 nicotinic acetylcholine receptor, demonstrates anxiolytic- and antidepressant-like effects in rodents

    Article • Neuropharmacology, March 2024, Elsevier

    Dr Brad E Sleebs

  16. Novel aroyl guanidine anti-trypanosomal compounds that exert opposing effects on parasite energy metabolism

    Article • European Journal of Medicinal Chemistry, March 2024, Elsevier

    Dr Brad E Sleebs

  17. Structure activity relationship and target prediction for ABX464 analogues in Caenorhabditis elegans

    Article • Bioorganic & Medicinal Chemistry, January 2024, Elsevier

    Dr Brad E Sleebs

  18. Sequence elements within the PEXEL motif and its downstream region modulate PTEX‐dependent protein export in Plasmodium falciparum

    Article • Traffic, November 2023, Wiley

    Dr Brad E Sleebs

  19. A Pyridyl-Furan Series Developed from the Open Global Health Library Block Red Blood Cell Invasion and Protein Trafficking in Plasmodium falciparum through Potential Inhibition of the Parasite’s PI4KIIIB Enzyme

    Article • ACS Infectious Diseases, August 2023, American Chemical Society (ACS)

    Dr Brad E Sleebs

  20. Chemo‐proteomics in antimalarial target identification and engagement

    Article • Medicinal Research Reviews, May 2023, Wiley

    Dr Brad E Sleebs

  21. Sulfonylpiperazine compounds prevent Plasmodium falciparum invasion of red blood cells through interference with actin-1/profilin dynamics

    Article • PLoS Biology, April 2023, PLOS

    Dr Brad E Sleebs

  22. 7-N-Substituted-3-oxadiazole Quinolones with Potent Antimalarial Activity Target the Cytochrome bc1 Complex

    Article • ACS Infectious Diseases, February 2023, American Chemical Society (ACS)

    Dr Brad E Sleebs

  23. Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4

    Article • Journal of Medicinal Chemistry, February 2023, American Chemical Society (ACS)

    Dr Brad E Sleebs

  24. Design and characterization of a heterobifunctional degrader of KEAP1

    Article • Redox Biology, February 2023, Elsevier

    Dr Brad E Sleebs

  25. Targeting malaria parasites with novel derivatives of azithromycin

    Article • Frontiers in Cellular and Infection Microbiology, November 2022, Frontiers

    A/Prof Rietie Venter, Dr Brad E Sleebs, James Beeson

  26. Thermal proteome profiling reveals Haemonchus orphan protein HCO_011565 as a target of the nematocidal small molecule UMW-868

    Article • Frontiers in Pharmacology, October 2022, Frontiers

    Dr Brad E Sleebs

  27. The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria

    Article • ACS Medicinal Chemistry Letters, October 2022, American Chemical Society (ACS)

    Dr Brad E Sleebs

  28. Australian chemistry and drug discovery towards the development of antimalarials

    Article • Australian Journal of Chemistry, September 2022, CSIRO Publishing

    Dr Brad E Sleebs

  29. Substrate Peptidomimetic Inhibitors of P. falciparum Plasmepsin X with Potent Antimalarial Activity

    Article • ChemMedChem, August 2022, Wiley

    Dr Brad E Sleebs, Dr. Paola Favuzza

  30. The Medicines for Malaria Venture Malaria Box contains inhibitors of protein secretion in Plasmodium falciparum blood stage parasites

    Article • Traffic, August 2022, Wiley

    Dr Brad E Sleebs

  31. Basis for drug selectivity of plasmepsin IX and X inhibition in Plasmodium falciparum and vivax

    Article • Structure, July 2022, Elsevier

    Dr Brad E Sleebs, Dr. Paola Favuzza

  32. A revised mechanism for how Plasmodium falciparum recruits and exports proteins into its erythrocytic host cell

    Article • PLoS Pathogens, February 2022, PLOS

    Dr Brad E Sleebs

  33. A High-Throughput Phenotypic Screen of the ‘Pandemic Response Box’ Identifies a Quinoline Derivative with Significant Anthelmintic Activity

    Article • Pharmaceuticals, February 2022, MDPI AG

    Dr Brad E Sleebs

  34. Optimization of Phosphotyrosine Peptides that Target the SH2 Domain of SOCS1 and Block Substrate Ubiquitination

    Article • ACS Chemical Biology, January 2022, American Chemical Society (ACS)

    Dr Brad E Sleebs

  35. Hydroxychloroquine inhibits the mitochondrial antioxidant system in activated T cells

    Article • iScience, December 2021, Elsevier

    Dr Brad E Sleebs

  36. Property activity refinement of 2-anilino 4-amino substituted quinazolines as antimalarials with fast acting asexual parasite activity

    Article • Bioorganic Chemistry, December 2021, Elsevier

    Dr Brad E Sleebs, Dr. Paola Favuzza

  37. Optimisation of 2-(N-phenyl carboxamide) triazolopyrimidine antimalarials with moderate to slow acting erythrocytic stage activity

    Article • Bioorganic Chemistry, October 2021, Elsevier

    Dr Brad E Sleebs, Dr. Paola Favuzza

  38. A revised mechanism for how Plasmodium falciparum recruits and exports proteins into its erythrocytic host cell

    Article • September 2021, Cold Spring Harbor Laboratory Press

    Dr Brad E Sleebs

  39. High-Throughput Phenotypic Assay to Screen for Anthelmintic Activity on Haemonchus contortus

    Article • Pharmaceuticals, June 2021, MDPI AG

    Dr Brad E Sleebs

  40. Late Stage Phosphotyrosine Mimetic Functionalization of Peptides Employing Metallaphotoredox Catalysis

    Article • Organic Letters, May 2021, American Chemical Society (ACS)

    Dr Brad E Sleebs

  41. Three Small Molecule Entities (MPK18, MPK334 and YAK308) with Activity against Haemonchus contortus In Vitro

    Article • Molecules, May 2021, MDPI AG

    Dr Brad E Sleebs

  42. Development of an automated assay for accelerated in vitro detection of DNA adduct-inducing and crosslinking agents

    Article • Bioorganic & Medicinal Chemistry Letters, March 2021, Elsevier

    Dr Brad E Sleebs

  43. Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion

    Article • European Journal of Medicinal Chemistry, March 2021, Elsevier

    Dr Brad E Sleebs

  44. Optimization of Benzothiazole and Thiazole Hydrazones as Inhibitors of Schistosome BCL-2

    Article • ACS Infectious Diseases, February 2021, American Chemical Society (ACS)

    Dr Brad E Sleebs

  45. Advances in the discovery and development of anthelmintics by harnessing natural product scaffolds

    Article • January 2021, Elsevier

    Dr Brad E Sleebs

  46. Synthesis of Acyl Phosphoramidates Employing a Modified Staudinger Reaction

    Article • Organic Letters, December 2020, American Chemical Society (ACS)

    Dr Brad E Sleebs

  47. Development and application of a high-throughput screening assay for identification of small molecule inhibitors of the P. falciparum reticulocyte binding-like homologue 5 protein

    Article • International Journal for Parasitology Drugs and Drug Resistance, December 2020, Elsevier

    Dr Brad E Sleebs

  48. Retargeting azithromycin analogues to have dual-modality antimalarial activity

    Article • BMC Biology, September 2020, Springer Science + Business Media

    Dr Brad E Sleebs, James Beeson

  49. Optimization of 5-substituted thiazolyl ureas and 6-substituted imidazopyridines as potential HIV-1 latency reversing agents

    Article • European Journal of Medicinal Chemistry, June 2020, Elsevier

    Dr Brad E Sleebs

  50. Synthetic Kavalactone Analogues with Increased Potency and Selective Anthelmintic Activity against Larvae of Haemonchus contortus In Vitro

    Article • Molecules, April 2020, MDPI AG

    Dr Brad E Sleebs

  51. Dual Plasmepsin-Targeting Antimalarial Agents Disrupt Multiple Stages of the Malaria Parasite Life Cycle

    Article • Cell Host & Microbe, April 2020, Elsevier

    Dr Brad E Sleebs, Dr. Paola Favuzza

  52. Screening the Medicines for Malaria Venture Pathogen Box for invasion and egress inhibitors of the blood stage of Plasmodium falciparum reveals several inhibitory compounds

    Article • International Journal for Parasitology, March 2020, Elsevier

    Dr Brad E Sleebs

  53. Formaldehyde-activated WEHI-150 induces DNA interstrand crosslinks with unique structural features

    Article • Bioorganic & Medicinal Chemistry, February 2020, Elsevier

    Dr Brad E Sleebs

  54. Inhibition of Plasmepsin V Activity Blocks Plasmodium falciparum Gametocytogenesis and Transmission to Mosquitoes

    Article • Cell Reports, December 2019, Elsevier

    Dr Brad E Sleebs

  55. Screening the Medicines for Malaria Venture Pathogen Box for invasion and egress inhibitors of the blood stage of Plasmodium falciparum reveals several inhibitory compounds

    Article • September 2019, Cold Spring Harbor Laboratory Press

    Dr Brad E Sleebs

  56. The Development Process for Discovery and Clinical Advancement of Modern Antimalarials

    Article • Journal of Medicinal Chemistry, August 2019, American Chemical Society (ACS)

    Dr Brad E Sleebs

  57. An appraisal of natural products active against parasitic nematodes of animals

    Article • Parasites & Vectors, June 2019, Springer Science + Business Media

    Dr Brad E Sleebs

  58. Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models

    Article • Journal of Medicinal Chemistry, April 2019, American Chemical Society (ACS)

    Dr Brad E Sleebs

  59. Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Apicomplexan Parasites In Vitro and in a P. falciparum Humanized NOD-scid IL2Rγnull Mouse Model of Malaria

    Article • Antimicrobial Agents and Chemotherapy, December 2018, ASM Journals

    Dr Brad E Sleebs

  60. Enhanced antimalarial activity of plasmepsin V inhibitors by modification of the P 2 position of PEXEL peptidomimetics

    Article • European Journal of Medicinal Chemistry, June 2018, Elsevier

    Dr Brad E Sleebs

  61. Conversion of Bim-BH3 from Activator to Inhibitor of Bak through Structure-Based Design

    Article • Molecular Cell, November 2017, Elsevier

    Dr Brad E Sleebs

  62. Screening the Medicines for Malaria Venture Pathogen Box across Multiple Pathogens Reclassifies Starting Points for Open-Source Drug Discovery

    Article • Antimicrobial Agents and Chemotherapy, July 2017, ASM Journals

    Dr Brad E Sleebs

  63. Mefloquine targets the Plasmodium falciparum 80S ribosome to inhibit protein synthesis

    Article • Nature Microbiology, March 2017, Nature

    Dr Brad E Sleebs

  64. Optimization of 2-Anilino 4-Amino Substituted Quinazolines into Potent Antimalarial Agents with Oral in Vivo Activity

    Article • Journal of Medicinal Chemistry, January 2017, American Chemical Society (ACS)

    Dr Brad E Sleebs

  65. Analysis of Ca2 + mediated signaling regulating Toxoplasma infectivity reveals complex relationships between key molecules

    Article • Cellular Microbiology, January 2017, Wiley

    Dr Brad E Sleebs

  66. Exploration of the P 3 region of PEXEL peptidomimetics leads to a potent inhibitor of the Plasmodium protease, plasmepsin V

    Article • Bioorganic & Medicinal Chemistry, May 2016, Elsevier

    Dr Brad E Sleebs

  67. Synthesis of amino heterocycle aspartyl protease inhibitors

    Article • Organic & Biomolecular Chemistry, January 2016, Royal Society of Chemistry

    Dr Brad E Sleebs

  68. Reversible and formaldehyde-mediated covalent binding of a bis-amino mitoxantrone analogue to DNA

    Article • Organic & Biomolecular Chemistry, January 2016, Royal Society of Chemistry

    Dr Brad E Sleebs

  69. Isolation and structural analysis of the covalent adduct formed between a bis-amino mitoxantrone analogue and DNA: a pathway to major–minor groove cross-linked adducts

    Article • Organic & Biomolecular Chemistry, January 2016, Royal Society of Chemistry

    Dr Brad E Sleebs

  70. An aspartyl protease defines a novel pathway for export of Toxoplasma proteins into the host cell

    Article • eLife, November 2015, eLife

    Dr Brad E Sleebs

  71. HIV-1 and Human PEG10 Frameshift Elements Are Functionally Distinct and Distinguished by Novel Small Molecule Modulators

    Article • PLOS One, October 2015, PLOS

    Dr Brad E Sleebs

  72. Mitoxantrone, More than Just Another Topoisomerase II Poison

    Article • Medicinal Research Reviews, August 2015, Wiley

    Dr Brad E Sleebs

  73. Structural basis for plasmepsin V inhibition that blocks export of malaria proteins to human erythrocytes

    Article • Nature Structural & Molecular Biology, July 2015, Springer Science + Business Media

    Dr Brad E Sleebs

  74. Macrolides rapidly inhibit red blood cell invasion by the human malaria parasite, Plasmodium falciparum

    Article • BMC Biology, July 2015, Springer Science + Business Media

    Dr Brad E Sleebs, James Beeson

  75. The effect of N-methylation on transition state mimetic inhibitors of the Plasmodium protease, plasmepsin V

    Article • MedChemComm, January 2015, Royal Society of Chemistry

    Dr Brad E Sleebs

  76. Macrocyclic N-Methylated Cyclic Peptides and Depsipeptides

    Article • January 2015, Elsevier

    Dr Brad E Sleebs

  77. Discovery of a Potent and Selective BCL-X L Inhibitor with in Vivo Activity

    Article • ACS Medicinal Chemistry Letters, October 2014, American Chemical Society (ACS)

    Dr Brad E Sleebs

  78. Transition State Mimetics of the Plasmodium Export Element Are Potent Inhibitors of Plasmepsin V from P. falciparum and P. vivax

    Article • Journal of Medicinal Chemistry, September 2014, American Chemical Society (ACS)

    Dr Brad E Sleebs

  79. Inhibition of Plasmepsin V Activity Demonstrates Its Essential Role in Protein Export, PfEMP1 Display, and Survival of Malaria Parasites

    Article • PLoS Biology, July 2014, PLOS

    Dr Brad E Sleebs, Dr Lea K Barfod, Dr Philip J. Shaw

  80. Structure-Guided Rescaffolding of Selective Antagonists of BCL-X L

    Article • ACS Medicinal Chemistry Letters, June 2014, American Chemical Society (ACS)

    Dr Brad E Sleebs

  81. Stereoselective Synthesis and Application of β-Amino Ketones

    Article • Current Organic Chemistry, January 2014, Bentham Science Publishers

    Dr Brad E Sleebs

  82. Discovery of Potent and Selective Benzothiazole Hydrazone Inhibitors of Bcl-X L

    Article • Journal of Medicinal Chemistry, July 2013, American Chemical Society (ACS)

    Dr Brad E Sleebs

  83. Diastereoselective synthesis of cyclic β2,3-amino acids utilizing 4-substituted-1,3-oxazinan-6-ones

    Article • Tetrahedron, July 2013, Elsevier

    Dr Brad E Sleebs

  84. Structure-guided design of a selective BCL-XL inhibitor

    Article • Nature Chemical Biology, April 2013, Springer Science + Business Media

    Dr Brad E Sleebs

  85. Synthesis of N-Cbz-Substituted β3-Amino Ketones Utilizing 4-Substituted 1,3-Oxazinan-6-ones

    Article • Synlett, March 2013, Thieme Publishing Group

    Dr Brad E Sleebs

  86. A Mild Multistep Conversion of N-Protected α-Amino Acids into N-Protected β3-Amino Acids Utilizing the Nef Reaction

    Article • Synlett, March 2013, Thieme Publishing Group

    Dr Brad E Sleebs

  87. Role of Plasmepsin V in Export of Diverse Protein Families from the Plasmodium falciparum Exportome

    Article • Traffic, February 2013, Wiley

    Dr Brad E Sleebs

  88. Corrigendum to “Diastereoselective synthesis of highly functionalized β2,2,3-substituted amino acids from 4-substituted-1,3-oxazinan-6-ones” [Tetrahedron 68 (2012) 4745–4756]

    Article • Tetrahedron, September 2012, Elsevier

    Dr Brad E Sleebs

  89. Diastereoselective synthesis of highly functionalized β2,2,3-substituted amino acids from 4-substituted-1,3-oxazinan-6-ones

    Article • Tetrahedron, June 2012, Elsevier

    Professor Jonathan White, Dr Brad E Sleebs

  90. Corrigendum to “Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors” [Bioorg. Med. Chem. Lett. 21 (2011) 5992–5994]

    Article • Bioorganic & Medicinal Chemistry Letters, January 2012, Elsevier

    Dr Brad E Sleebs

  91. M2, a novel anthracenedione, elicits a potent DNA damage response that can be subverted through checkpoint kinase inhibition to generate mitotic catastrophe

    Article • Biochemical Pharmacology, December 2011, Elsevier

    Dr Brad E Sleebs

  92. Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors

    Article • Bioorganic & Medicinal Chemistry Letters, October 2011, Elsevier

    Dr Brad E Sleebs

  93. Quinazoline Sulfonamides as Dual Binders of the Proteins B-Cell Lymphoma 2 and B-Cell Lymphoma Extra Long with Potent Proapoptotic Cell-Based Activity

    Article • Journal of Medicinal Chemistry, March 2011, American Chemical Society (ACS)

    Dr Brad E Sleebs

  94. Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors

    Article • MedChemComm, January 2011, Royal Society of Chemistry

    Dr Brad E Sleebs

  95. Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors

    Article • MedChemComm, January 2011, Royal Society of Chemistry

    Dr Brad E Sleebs

  96. New Anthracenedione Derivatives with Improved Biological Activity by Virtue of Stable Drug−DNA Adduct Formation

    Article • Journal of Medicinal Chemistry, October 2010, American Chemical Society (ACS)

    Dr Brad E Sleebs

  97. De Novo Synthesis of a Potent LIMK1 Inhibitor

    Article • Synthesis, January 2010, Thieme Publishing Group

    Dr Brad E Sleebs

  98. Recent Advances in Stereoselective Synthesis and Application of β-Amino Acids

    Article • Organic Preparations and Procedures International, November 2009, Taylor & Francis

    Dr Brad E Sleebs

  99. Conformational Changes in Bcl-2 Pro-survival Proteins Determine Their Capacity to Bind Ligands

    Article • Journal of Biological Chemistry, September 2009, American Society for Biochemistry & Molecular Biology (ASBMB)

    Dr Brad E Sleebs

  100. Studies of 2-Substituted 1,3-Oxazolidin-5-ones and 1,3-Oxazinan-6-ones as Precursors for the Synthesis ofN-Alkyl-β-Amino Acids

    Article • Synthetic Communications, December 2008, Taylor & Francis

    Dr Brad E Sleebs

  101. Exploitation of the Arndt-Eistert Homologation of N-Methyl-�-Amino Acids for Concomitant Ester and N-Methyl Peptide Formation

    Article • Australian Journal of Chemistry, January 2008, CSIRO Publishing

    Dr Brad E Sleebs

  102. Diastereoselective Synthesis of α-Methyl and α-Hydroxy-β-Amino Acids via 4-Substituted-1,3-Oxazinan-6-ones

    Article • The Journal of Organic Chemistry, April 2007, American Chemical Society (ACS)

    Dr Brad E Sleebs

  103. Effective Methods for the Synthesis ofN-Methylβ-Amino Acids from All Twenty Commonα-Amino Acids Using 1,3-Oxazolidin-5-ones and 1,3-Oxazinan-6-ones

    Article • Helvetica Chimica Acta, November 2006, Wiley

    Dr Brad E Sleebs

  104. Synthesis of New β-Amino Acids via 5-Oxazolidinones and the Arndt–Eistert Procedure

    Article • Australian Journal of Chemistry, January 2005, CSIRO Publishing

    Dr Brad E Sleebs