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Overview

Our research is a at the interface of medicinal chemistry and chemical biology, focusing on Malaria, Tuberculosis and Schistosomiasis. Our hypothesis-driven research is carried out in the context of integrated drug discovery incorporating a wide range of disciplines including pre-clinical pharmacology, biology, computer-aided drug discovery (CADD), drug metabolism and pharmacokinetics (DMPK), biotransformation, toxicology, target deconvolution as well as pharmaceutical sciences through supramolecular beneficiation of drug leads to improve physicochemical properties. These are available in-house and accessible through collaborations with H3D Drug Development Centre [http://www.h3d.uct.ac.za/], Prof. Timothy Egan & Prof. Mino Caira (University of Cape Town), Dr. Sergio Wittlin and Prof. Jenny Keiser (Swiss Tropical & Public Health Institute, [https://www.swisstph.ch/en/]),  Prof. Lyn-Marie Birkholtz (University of Pretoria, [https://www.up.ac.za/the-genomics-research-institute/article/1928955/professor-lyn-marie-birkholtz) and Dr. David Fidock (Columbia University, [https://www.fidock.org/]). Our drug discovery research is based on the optimization of chemical matter hits arising from both target-based (i.e. Protein Kinase, Co-Enzyme A Biosynthesis and Hemozoin Formation Inhibitors etc.) and phenotypic whole cell-based screening campaigns. Other approaches include repositioning and utilization of privileged scaffolds as molecular starting points. Prof. Kelly Chibale’s (KC) earlier work included asymmetric synthesis utilizing sulfur and organolanthanide chemistry as well as the total synthesis of natural and designed biologically relevant molecules