Brad Sleebs

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

William Nguyen, Erinna F Lee, Marco Evangelista, Mihwa Lee, Tiffany J Harris, Peter M Colman, Nicholas A Smith, Luke B Williams, Kate E Jarman, Kym N Lowes, Cécile Haeberli, Jennifer Keiser, Brian J Smith, W Douglas Fairlie, Brad E Sleebs

Journal article  |  2021  |  ACS Infectious Diseases

Limited therapeutic options are available for the treatment of human schistosomiasis caused by the parasitic Schistosoma flatworm...

Synthesis of Acyl Phosphoramidates Employing a Modified Staudinger Reaction.

Iain Currie, Brad E Sleebs

Journal article  |  2021  |  Organic Letters

A one-step synthesis of acyl phosphoramidates from a variety of functionalized acyl azides has been developed employing trimethyls..

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

HMP Dilrukshi Herath, Aya C Taki, Brad E Sleebs, Andreas Hofmann, Nghi Nguyen, Sarah Preston, Rohan A Davis, Abdul Jabbar, Robin B Gasser

Journal article  |  2021  |  Advances in parasitology

Widespread resistance to currently-used anthelmintics represents a major obstacle to controlling parasitic nematodes of livestock ..

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

Brad E Sleebs, Kate E Jarman, Sonja Frolich, Wilson Wong, Julie Healer, Weiwen Dai, Isabelle S Lucet, Danny W Wilson, Alan F Cowman

Journal article  |  2020  |  International Journal for Parasitology: Drugs and Drug Resistance

The P. falciparum parasite, responsible for the disease in humans known as malaria, must invade erythrocytes to provide an environ..

Retargeting azithromycin analogues to have dual-modality antimalarial activity

Amy L Burns, Brad E Sleebs, Ghizal Siddiqui, Amanda E De Paoli, Dovile Anderson, Benjamin Liffner, Richard Harvey, James G Beeson, Darren J Creek, Christopher D Goodman, Geoffrey I McFadden, Danny W Wilson

Journal article  |  2020  |  BMC Biology

Background Resistance to front-line antimalarials (artemisinin combination therapies) is spreading, and development of new drug tr..

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

William Nguyen, Jonathan Jacobson, Kate E Jarman, Timothy R Blackmore, Helene Jousset Sabroux, Sharon R Lewin, Damian F Purcell, Brad E Sleebs

Journal article  |  2020  |  European Journal of Medicinal Chemistry

A persistent latent reservoir of virus in CD4+ T cells is a major barrier to cure HIV. Activating viral transcription in latently ..

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

Paola Favuzza, Manuel de Lera Ruiz, Jennifer K Thompson, Tony Triglia, Anna Ngo, Ryan WJ Steel, Marissa Vavrek, Janni Christensen, Julie Healer, Christopher Boyce, Zhuyan Guo, Mengwei Hu, Tanweer Khan, Nicholas Murgolo, Lianyun Zhao, Jocelyn Sietsma Penington, Kitsanapong Reaksudsan, Kate Jarman, Melanie H Dietrich, Lachlan Richardson, et al.

Journal article  |  2020  |  Cell Host & Microbe

Artemisin combination therapy (ACT) is the main treatment option for malaria, which is caused by the intracellular parasite Plasmo..

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

HMP Dilrukshi Herath, Aya C Taki, Nguyen Nghi, Jose Garcia-Bustos, Andreas Hofmann, Tao Wang, Guangxu Ma, Bill CH Chang, Abdul Jabbar, Brad E Sleebs, Robin B Gasser

Journal article  |  2020  |  Molecules

Kava extract, an aqueous rhizome emulsion of the plant Piper methysticum, has been used for centuries by Pacific Islanders as a ce..

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

Madeline G Dans, Greta E Weiss, Danny W Wilson, Brad E Sleebs, Brendan S Crabb, Tania F de Koning-Ward, Paul R Gilson

Journal article  |  2020  |  International Journal for Parasitology

With emerging resistance to frontline treatments, it is vital that new drugs are identified to target Plasmodium falciparum. One o..

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

Paul P Pumuye, Benny J Evison, Shyam K Konda, J Grant Collins, Celine Kelso, Jelena Medan, Brad E Sleebs, Keith Watson, Don R Phillips, Suzanne M Cutts

Journal article  |  2020  |  Bioorganic & Medicinal Chemistry

Mitoxantrone is an anticancer anthracenedione that can be activated by formaldehyde to generate covalent drug-DNA adducts. Despite..