Design and synthesis of selective kinase inhibitors
Project type
Honours and/or PhD
| Supervisor(s) | Division | |
| (Primary) | Chemical Biology | .(JavaScript must be enabled to view this email address) |
| (Co-supervisor) | Chemical Biology | .(JavaScript must be enabled to view this email address) |
Details of project
This project is focused on the design of small molecule inhibitors of specific kinases known to drive cancer cell growth, and builds on preliminary data obtained in our lab and published work. Thus chemistry methods have been established to synthesise an array of compounds to understand the structural features required for compound potency and selectivity.
All compounds prepared will be tested in biological assays to determine the activity of the compounds against the specific target kinases. Further optimisation of these compounds would seek to improve their potency, selectivity and metabolic stability, with the aim of developing compounds that could be tested in specific in vivo models of cancer with the ultimate aim of discovering a drug for clinical development.
Research interests
Our research interests are in the design and synthesis of novel chemical compounds with potent biological activity against targets implicated in cancer. Such compounds have the potential to be developed as anti-cancer drugs, and to help unravel the complex signaling processes present in cancer cells.
The compounds are designed using a combination of rational drug design principles and careful analysis of structure-activity relationships, whilst ensuring the compounds have appropriate metabolic stability and oral activity (i.e. can be dosed as a pill).
Selected publications
- Burns CJ et al. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorg Med Chem Lett. 2009;19:5887.
- Burns CJ et al. CYT997: a novel oral vascular disrupting agent with potent antitumour activity in vivo. Mol. Cancer Ther. 2009;8:3036.
Research theme
Cancer
Scientific discipline
- Medicinal Chemistry
Keywords
drug design, synthesis, kinase inhibitors