Synthesis of the pyrrolo[2,1-c][1,4]benzodiazepines: potent DNA binders. Chemicals that bind to DNA have a long history of use as anticancer drugs. In recent times, the biotechnology revolution has greatly expanded our understanding of how these drugs work and the genetic basis of a wide range of other diseases. The aim of this project is to discover novel compounds that selectively bind to DNA. Starting from a class of naturally occurring compounds (called the pyrrolobenzodiazepines) as a templ ....Synthesis of the pyrrolo[2,1-c][1,4]benzodiazepines: potent DNA binders. Chemicals that bind to DNA have a long history of use as anticancer drugs. In recent times, the biotechnology revolution has greatly expanded our understanding of how these drugs work and the genetic basis of a wide range of other diseases. The aim of this project is to discover novel compounds that selectively bind to DNA. Starting from a class of naturally occurring compounds (called the pyrrolobenzodiazepines) as a template, it will develop powerful new methods to supply wholly new DNA interactive molecules with great potential as new drugs to treat cancer or other genetic diseases.Read moreRead less
Anti-Cancer Natural Products: Total Synthesis and Biological Evaluation of Lasonolide A and Analogues. One in three men and one in four women in Australia will be diagnosed with cancer before they reach 75. Cancer is a leading cause of death within this country with 28% of deaths each year due to this disease. Although there have been advances in the treatment of various forms of cancer there remains a pressing need for new therapies with improved potency, selectivity and reduced side effects. T ....Anti-Cancer Natural Products: Total Synthesis and Biological Evaluation of Lasonolide A and Analogues. One in three men and one in four women in Australia will be diagnosed with cancer before they reach 75. Cancer is a leading cause of death within this country with 28% of deaths each year due to this disease. Although there have been advances in the treatment of various forms of cancer there remains a pressing need for new therapies with improved potency, selectivity and reduced side effects. This project will provide new compounds of potential clinical use in the treatment of cancer, thereby aiding the large population of Australians who will be affected by this disease. Furthermore, the new advanced materials produced by this project will aid in the study of biochemical processes involved in cancer.Read moreRead less
High Pressure and Fluorous Approaches to Fostriecin Libraries: New Therapeutic Opportunities. The natural product, Fostriecin, displays considerable broad-spectrum anti-cancer activity, acting via a novel mechanism. However, this activity is tempered by its considerable instability, being too unstable to be used as a therapeutic agent. Using state-of-the-art approaches we will, rapidly generate libraries of more stable and biologically active fostriecin analogues and examine their potential to b ....High Pressure and Fluorous Approaches to Fostriecin Libraries: New Therapeutic Opportunities. The natural product, Fostriecin, displays considerable broad-spectrum anti-cancer activity, acting via a novel mechanism. However, this activity is tempered by its considerable instability, being too unstable to be used as a therapeutic agent. Using state-of-the-art approaches we will, rapidly generate libraries of more stable and biologically active fostriecin analogues and examine their potential to be used anti-cancer agents. This project represents an opportunity for Australia to take a significant, innovative lead in the development of hitherto unforseen therapeutic agents.Read moreRead less
New methods for the chemical synthesis of a library of glycopeptide-based tri-component cancer vaccines. A novel method for the synthesis of tumour-associated glycopeptides will be developed in this research as well as the preparation of a library of glycopeptide-based cancer vaccines. These vaccines will be tested in immunological studies with a view to elucidating new immune-based therapies for the treatment of cancer.
Discovery Early Career Researcher Award - Grant ID: DE140101632
Funder
Australian Research Council
Funding Amount
$395,220.00
Summary
Development of Innovative Chemical Tools for Studying Glycosyltransferases . This project aims to develop chemical probes capable of selectively binding and inhibiting two classes of carbohydrate processing enzymes known as O-linked beta-N-acetylglucosamine transferase and sialyltransferases. These enzymes are overexpressed in various cancers and play critical roles in cancer progression. Probes will be developed to analyse the activities of these enzymes in cancer cells.
Discovery Early Career Researcher Award - Grant ID: DE130101673
Funder
Australian Research Council
Funding Amount
$375,000.00
Summary
Access to biomimetic carbohydrate receptors using dynamic combinatorial chemistry. This project aims to utilise novel synthetic technology for the development of cyclic peptide libraries as novel drug leads for the treatment of Dengue virus, HIV and cancer.
Discovery Early Career Researcher Award - Grant ID: DE120101653
Funder
Australian Research Council
Funding Amount
$375,000.00
Summary
Selective fluorination chemistry: a tool for creating bioactive, shape-controlled peptides. Fluorine atoms are desirable substituents in drug candidates because they can increase metabolic stability and hydrophobicity, and because they can be used to constrain molecules into optimal bioactive conformations. These concepts are being exploited to create shape-controlled peptides with applications in anti-cancer and anti-microbial therapy.