Our current medicinal chemistry programme on anti-infective (anti-malarial, anti-tuberculosis, anti-HIV/AIDS), anti-hypertension and anti-cancer agents has three main objectives:
- to develop target-directed inhibitors
- to develop single agents that provide target-directed inhibition of multiple disease-causing organisms or cells
- to develop single agents that provide maximal anti-infective and anti-cancer activity by acting against multiple targets.
More recently, we have initiated a major research programme aimed at integrating African natural products and biodiversity research into modern drug discovery paradigms. This project is partly under the auspices of the Medical Research Council (MRC) Drug Discovery and Development Research Unit (http://www.mrc.ac.za/drug/drug.htm). Specifically we are creating a technology platform that will allow the exploration of the potential of African natural products and general biodiversity to feed into modern paradigms of drug discovery in the form of a virtual database and actual physical collection of purified and characterized African natural products. We are pursuing virtual (in silico) screening of African natural product libraries against novel and validated molecular targets of infectious diseases. As part of a programme to diversify and enrich the collection of purified African natural products, we have set up a biotransformation platform for combinatorial biocatalysis mediated by a panel of recombinant bacterial and human cytochrome P450s.
Kelly Chibale’s earlier work has included asymmetric synthesis utilizing sulfur and organolanthanide chemistry as well as the total synthesis of natural and designed biologically relevant molecules.
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