Prof Kelly Chibale
Our current medicinal chemistry programme against the causative agents of malaria, tuberculosis and helminth infections on one hand, and cardiovascular disease on the other, has four main objectives:
- To develop target–directed inhibitors.
- Progress hits from target– and phenotypic whole cell–based high throughput screening campaigns to deliver leads suitable for optimization and ultimately candidate selection.
- To generate diversity in complex natural products through semi-synthesis and use of biotransformation.
- To employ biotransformation in the generation and characterization of pharmacologically active and potentially toxic reactive metabolites of drugs and drug leads.
- To repurpose/reposition and rescue clinical compounds.
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.
(Full list of publications to be found at http://www.kellychibale-researchgroup-uct.com/publications/)
- Purification of human malaria parasite hypoxanthine guanine xanthine phosphoribosyltransferase (HGXPRT) using immobilized Reactive Red 120. B. Mbewe, K. Chibale and D. B. McIntosh. Protein Expression and Purification , 2007, 52, 153-158.
- Antiplasmodial hirsutinolides from Vernonia staehelinoides and their utilization towards a novel simplified pharmacophore. P. Pillay, R. Vleggaar, V. J. Maharaj, P. J. Smith, C. A. Lategan,. F.
- Studies in Iridoid Synthesis. Chemoselective Transformations of Cis-1,2,4,6-Tetrahydrophthalic Anhydride. A. T. Stevens, J. R. Bull and K. Chibale. Org. Biomol. Chem., 2008, 6, 586-595.
- Synthesis, Antimalarial and Antitubercular Activity of Acetylenic Chalcones. R.H. Hans, E.M Guantai, C. Lategan, P.J Smith, B. Wan, S.G Franzblau, J. Gut, P. J Rosenthal and K. Chibale. Bioorg. Med. Chem. Lett., 2010, 20, 942-944.
- Identification and characterization of reactive metabolites in natural products driven drug discovery. N. M. Njuguna. C. Masimirembwa and K. Chibale. J. Nat. Prod., 2012, 75, 507-513.
- 3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential. Y. Younis, F. Douelle, T.–S.Feng, D. González Cabrera, C. Le Manach, A. T. Nchinda, S. Duffy, K. L. White, D. M. Shackleford, J. Morizzi,J. Mannila, K. Katneni,R. Bhamidipati,K. M. Zabiulla, J. T. Joseph, S. Bashyam, D. Waterson, M. J. Witty, D. Hardick, S. Wittlin, V. Avery, S. A. Charman and K. Chibale. J. Med. Chem., 2012, 55, 3479−3487.
- A new approach for anthelmintic discovery for humans. T.G. Geary, K. Chibale, B. Abegaz, K. Andrae–Marobela and E. Ubalijoro. Trends in Parasitology, 2012, 28(5), 176-181.
- New ketomethylene inhibitor analogues: Synthesis and assessment of structural determinants for N-domain selective inhibition of angiotensin-converting enzyme. R. K. Sharma, R. G. Douglas, S. Louw, K. Chibale and E. D. Sturrock. Biological Chemistry, 2012, 393, 485-494.
- Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS–Malaria combination therapy. M.N. Aminake, A. Mahajan, V. Kumar, R. Hans, L. Wiesner, D. Taylor, C. de Kock, A. Grobler, P.J. Smith, M. Kirschner, A. Rethwilm, G. Pradel and K. Chibale. Bioorg. Med. Chem., 2012, 20, 277–5289.
- The comparison of ESI, APCI and APPI for the identification of metabolites from labile artemisinin-based anti-malarial drugs using a Q TRAP mass spectrometer. S. Louw, M. Njoroge, N. Chigorimbo-Murefu and K. Chibale. Rapid Commun. Mass Spectrom., 2012, 26, 2431–2442.