[116] Structure-Activity Relationship Studies of Orally active Antimalarial 3,5-Substituted 2-Aminopyridines. D. González Cabrera, F. Douelle, Y. Younis, T.-S. Feng, C. LeManach, A. Nchinda, L. Street, C. Scheurer, J. Kamber, K. White, O. Montagnat, E. Ryan, K. Katneni, K. M. Zabiulla, J. Joseph, S. Bashyam, D. Waterson, M. Witty, S. Charman, S. Wittlin, and K. Chibale* J. Med. Chem.  2012, 55, 11022– 11030
[115] Antimalarial aminothiazoles and aminopyridines from phenotypic whole cell screening of a SoftFocus library. T. Paquet, R. Gordon, D. Waterson, M. J. Witty, and K. Chibale* Future Med. Chem. 2012, 4(18), 2265–2277


Biotransformation and Biocatalysis: roles and applications in the discovery of antimalarials. N. T. L. Chigorimbo-Murefu, M. Njoroge, A. Nzila, S. Louw, C. Masimirembwa and K. Chibale* Future Med. Chem. 2012, 4(18), 2325-2336.


The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives. M. Tukulula, S. Little, J. Gut, P.J. Rosenthal, B. Wan, S. G. Franzblau and K. Chibale*. Eur. J. Med. Chem. 2012, 57, 259-267.


Artemisinin derivatives: a patent review (2006 - present) N. Njuguna, D.S.B. Ongarora and K. Chibale* Expert Opinion in Therapeutic Patents. 2012, 22(10), 1179-1203.


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.


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, 5277-5289.


Benzoheterocyclic Amodiaquine Analogues with Potent Antiplasmodial Activity: Synthesis and Pharmacological Evaluation. D.S.B. Ongarora, J. Gut, P.J. Rosenthal, C.M. Masimirembwa, and K. Chibale.* Bioorg. Med. Chem. Lett. 2012, 22, 5046-5050.


Exploring the Versatility of Cycloplatinated Thiosemicarbazones as Antitumour and Antiparasitic Agents. P. Chellan, K.M. Land, A. Shokar, A. Au, S. H. An, C. M.Clavel, P. J. Dyson, C. de Kock, P.J. Smith, K. Chibale and G.S. Smith* Organometallics 2012, 31, 5791−5799.


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(6), 485-494.


Potent inhibition of CYP1A2 by Frutinone A, an active ingredient of the broad spectrum antimicrobial herbal extract from P. fruticosa. R. Thelingwani, K. Dhansay, P. J. Smith, K. Chibale and C.M. Masimirembwa* Xenobiotica, 2012, 1-12.


2-Aminopyrimidine based 4-aminoquinoline antiplasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies. K. Singh, H. Kaur, K. Chibale, J. Balzarini, S. Little and P.V.Bharatam Eur. J. Med. Chem. 2012, 52, 82-97.


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.

[103] 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


Synthesis of Aminoquinoline-Based Aminoalcohols and Oxazolidinones and Their Antiplasmodial Activity. F. Kobarfard, V. Yardley, S. Little, F. Daryaee and K. Chibale. Chem Biol Drug Des 2012; 79: 326-331.


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.


Synthesis, Biological Evaluation and Mechanistic Studies of Totarol Amino Alcohol Derivatives as Potential Antimalarial Agents. C. Tacon, E.M. Guantai, P. J. Smith, and K. Chibale* Bioorg. Med. Chem. 2012, 20, 893-902.