Characterisation and Development of Dynamic Supramolecular Combinatorial Libraries. The discovery of biologically active molecules, in particular drug discovery, requires the design and synthesis of host molecules that bind selectively to the biological target. Combinatorial chemistry has greatly assisted this discovery process as it allows the rapid screening of large collections of molecules. In this proposal, metal ion interactions will be used in the combinatorial library as this will grea ....Characterisation and Development of Dynamic Supramolecular Combinatorial Libraries. The discovery of biologically active molecules, in particular drug discovery, requires the design and synthesis of host molecules that bind selectively to the biological target. Combinatorial chemistry has greatly assisted this discovery process as it allows the rapid screening of large collections of molecules. In this proposal, metal ion interactions will be used in the combinatorial library as this will greatly increases the diversity of the pool of compounds to be screened for activity. Understanding how to generate and analyze these libraries has potential applications in drug screening, the discovery of new substrates, enzymes and inhibitors. Read moreRead less
Synthesis of Bioactive Metabolites from Myxobacteria. The crocacins and apicularens are two diverse groups of biologically active molecules isolated from myxobacteria. Crocacins A-D are dipeptides which show antifungal activity and are highly cytostatic in mammalian cell cultures. The novel macrolide apicularen A is highly active against a number of human tumour cell lines and shows promise as a new type of anticancer compound. The aim of this project is develop a methodology to synthesise these ....Synthesis of Bioactive Metabolites from Myxobacteria. The crocacins and apicularens are two diverse groups of biologically active molecules isolated from myxobacteria. Crocacins A-D are dipeptides which show antifungal activity and are highly cytostatic in mammalian cell cultures. The novel macrolide apicularen A is highly active against a number of human tumour cell lines and shows promise as a new type of anticancer compound. The aim of this project is develop a methodology to synthesise these novel compounds.Read moreRead less
Enabling Methodologies for the Synthesis of Biologically Active Compounds. This project seeks to establish flexible methods of chemical synthesis for creating new molecular scaffolds capable of achieving selective enzyme inhibition. The approach aims to exploit the vast and biologically-programmed structural diversity associated with natural products. Unique, small molecule organic compounds will be obtained that reveal details of the operation of key enzymes in bacterial and mammalian systems. ....Enabling Methodologies for the Synthesis of Biologically Active Compounds. This project seeks to establish flexible methods of chemical synthesis for creating new molecular scaffolds capable of achieving selective enzyme inhibition. The approach aims to exploit the vast and biologically-programmed structural diversity associated with natural products. Unique, small molecule organic compounds will be obtained that reveal details of the operation of key enzymes in bacterial and mammalian systems. Such new knowledge would allow for the design of highly selective therapeutic agents relevant to the treatment of a range of diseases including bacterial infections, diabetes and cancer. The high-end scientific training and privileged forms of matter arising from this work would provide major benefit to the biotech sector.Read moreRead less