Publications

Book Chapters

[1].       Contributed to World Health Organization (WHO), Geneva, Switzerland, book chapter entitled “Enabling innovation” prepared for publication in the book entitled “Combating Antimicrobial Resistance: Experiences from the Field”  planned to appear as a WHO book publication in 2011.[2].       E. M. Guantai and K. Chibale. (2012) ‘Natural product-based drug discovery in Africa: the need for integration into modern drug-discovery paradigms. In: Drug Discovery in Africa, eds. Chibale K., Masimirembwa C. and Davies-Coleman, M., Springer: Germany (2012).

[3].       A. Nzila and K. Chibale. (2012) ‘Anticancer drug repositioning against tropical diseases: the example of methotrexate in the treatment of malaria’. In: Drug Discovery in Africa, eds. Chibale K., Masimirembwa C. and Davies-Coleman, M., Springer: Germany (2012).

[4].       N.T. L Chigorimbo-Murefu, G. Mugumbate and K. Chibale (2013), ‘Enabling Technologies to facilitate natural product-based drug discovery from African Biodiversity. In: Novel Plant Bioresources, eds. Gurib-Fakim, A., Wiley: country (2014), in press.

[5].       P.N. Njogu and K. Chibale* (2014), ‘Current and future strategies for improving drug discovery efficiency. In: XX, eds. Alexander, A., Smith, D.A.; Harris, C.J.,  X: country (2014), in press.

Papers in refereed journals as of June 2014 (Excluding Papers in Preparation)

NOTE: An asterisk (*) indicates the principal/lead author(s) regardless of position/number where name(s) appear on a particular paper.  Due to the multi-disciplinary nature of the research I do, there is not a single uniform agreed upon format for indicating authorship and this indeed tends to vary depending on the collaboration. However, more recently on papers where I am the principal/lead author, I tend to put my name last and the name of the student who did most of the work in the lab first. 

 JIF = Journal Impact Factor

[1]       Asymmetris Synthesis of Spirocyclic Pyrrolidines and Tetrahydrofurans by Chiral Aldol   Reactions and Phenylthio Migration.  K. Chibale and S. Warren*. Tetrahedron Lett., 1991, 32, 6645-6648. JIF = 2.50

[2]       Kinetic Resolutions in Anti Aldol Reactions with Racemic 2-Phenylthio      Aldehydes:  Asymmetric Synthesis of Cyclic Ethers and Lactones with Phenylthio Migration.  K. Chibale     and S. Warren*. Tetrahedron Lett., 1992, 33, 4369-4372.   JIF = 2.50

[3]        Kinetic Resolutions in Anti Aldol Reactions:  Asymmetric Synthesis of Heterocycles with Phenylthio Migration.  K. Chibale and S. Warren*. Phosphorus, Sulfur & Silicon, 1993, 74, 401-402.  JIF = 0.515

[4]        The Stereochemically Controlled Synthesis of Spirocyclic Ethers and Lactones with Medium-Sized (7-, 8- and 12-Membered) Carbocyclic Rings by Phenylthio Migration:  1-Oxaspiro[4.n]alkanes and Alkan-2-ones with n = 6,7, and 11.  K. Chibale, R.C. Hartley, K.P. Jenkins, M. Simons, S. Warren* and I.C. Richards. Tetrahedron Lett., 1993, 34, 6783-6786.  JIF = 2.50

[5]        New Homochiral Binaphthol-Modified Organolanthanide Reagents for the Enantioselective Addition to Aldehydes.  K. Chibale, N. Greeves*, L. Lyford and E. J. Pease. Tetrahedron: Asymmetry 1993, 4, 2407-2410.   JIF = 2.53

[6]       The Synthesis of Optically Active 2-Phenylthio Aldehydes.  K. Chibale and S. Warren*.   Tetrahedron Lett., 1994, 35, 3991-3994.  JIF =2.50

[7]        Asymmetric Aldol Reactions of Achiral 2-Phenylsulfanyl Aldehydes with Small   (5- and 6-Membered) and Medium-Sized (8- and 12-Membered) Carbocyclic Rings: The Synthesis of Homochiral Spirocyclic Lactones, Pyrrolidines and Tetrahydrofurans. K. Chibale and S. Warren*. J. Chem. Soc., Perkin Trans.1, 1995, 2411-2418.  JIF = 2.2

[8]        Kinetic Resolution in Asymmetric Anti Aldol Reactions of Branched and Straight Chain Racemic 2-Phenylsulfanyl Aldehydes:  Asymmetric Synthesis of Cyclic Ethers and Lactones by     Phenylsulfanyl Migration.  K. Chibale and S. Warren*. J. Chem. Soc., Perkin Trans.1, 1996,         1935-1940.  JIF = 2.2

[9]       Design, Synthesis and Biological Evaluation of Carbohydrate-Based Mimetics of cRGDFV.  K.C. Nicolaou*, J.I. Trujillo and K. Chibale. Tetrahedron 1997, 53, 8751-8778.   JIF =3.01

[10]      Design, Synthesis and Biological Evaluation of Nonpeptide Integrin Antagonists .   K.C. Nicolaou*, J.I. Trujillo, B. Jandeleit, K. Chibale, M. Rosenfeld, B. Diefenbach, D.A. Cheresh and S.L. Goodman. Bioorg. Med. Chem, 1998, 6, 1185-1208.   JIF =3.04

[11]      Synthesis and Evaluation of 9,9-Dimethylxanthene Tricyclics Against Trypanothione Reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani. K. Chibale*, M. Visser, V. Yardley, S.L. Croft and A.H. Fairlamb. Bioorg. Med. Chem, Letts 2000, 10, 1147-1150.   JIF =2.59

[12]      New Amine and Urea Analogs of Ferrochloroquine: Synthesis, Antimalarial Activity In Vitro and Electrochemical Studies. K. Chibale*, J.R. Moss, M. Blackie, D. van Schalkwyk and P.J. Smith. Tetrahedron Letts 2000, 41, 6231-6235.  JIF =2.50

[13]      Modulation of Human Mammary Cell Sensitivity to Paclitaxel by New Quinoline Sulfonamides. K. Chibale*, I. Ojima, H. Haupt, X. Geng, P. Pera and R. J. Bernacki. Bioorg. Med. Chem. Letts. 2001, 11, 2457-2460.   JIF =2.59

[14]      Antiprotozoal and Cytotoxicity Evaluation of Sulfonamide and Urea Analogs of Quinacrine. K. Chibale*, H. Haupt, H. Kendrick, V. Yardley, A. Saravanamuthu, A.H. Fairlamb and S.L. Croft. Bioorg. Med. Chem. Letts. 2001, 11, 2655-2657.  JIF =2.59

[15]      A Novel and Efficient Regiospecific Preparation of Arenesulfonamide Derivatives of 3,5-Diamino-1,2,4-triazole. K. Chibale*, J. Dauvergne and P. J. Wyatt. Synthesis, 2002, 185- 190  JIF = 2.4

[16]      Convenient synthesis of disulfide substrates for trypanothione reductase using polymer-supported reagents.  K. Chibale*, A. Chipeleme and S. Warren.  Tetrahedron Lett., 2002, 43(8), 1587-1589.  JIF=2.50

[17]      A Chemical Approach towards Understanding the Mechanism and Reversal of Drug Resistance in Plasmodium falciparum: Is it Viable? K. Chibale*. International Union of Biochemistry and Molecular Biology (IUBMB) Life, 2002, 53, 249-252.   JIF =2.91

[18]      Synthesis and antimalarial activity in vitro of new ruthenocene-chloroquine analogues.  P. Beagley, M. A. L. Blackie, K. Chibale*, C. Clarkson, J. R. Moss* and P. J. Smith.  J. Chem. Soc., Dalton. Trans., 2002, 4426-4433.   JIF =3.93

[19]      Towards broadspectrum antiparasitic agents, K. Chibale*, ARKIVOC, 2002, (ix), 93-98  JIF =1.21

[20]      Design, synthesis, and evaluation of taxanes as potential antimalarial agents. J Chen, L Kuznetsova, K Chibale, I Ojima et al.  Abstracts of Papers of the American Chemical Society   2003, 226, U48-U48  JIF = 8.80

[21]      Exploring the potential of xanthene derivatives as trypanothione reductase inhibitors and chloroquine potentiating agents.  K. Chibale*, M. R. Visser, D. van Schalkwyk, P. J. Smith, A. Saravanamuthu and A. H. Fairlamb. Tetrahedron, 2003, 59, 2289-2296.   JIF =3.04

[22]      The synthesis of parasitic cysteine protease and trypanothione reductase inhibitors. K. Chibale* and C. C. Musonda.  Curr. Med. Chem. 2003, 10, 1863-1889.   JIF =5.38

[23]      Synthesis and Antiplasmodial Activity in vitro of New Ferrocene-chloroquine Analogues.  P. Beagley, M. A. L. Blackie, K. Chibale,* C. Clarkson, R. Meijboom, J. R. Moss,* P. J. Smith and H. Su. Dalton Transactions, 2003, 3046- 3051.   JIF =3.93

[24]      Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.  I. Chiyanzu, E. Hansell, J. Gut, P. J. Rosenthal, J. H. McKerrow and K. Chibale*. Bioorg. Med. Chem. Letts. 2003. 13, 3527-3530.  JIF =2.59

[25]      Synthesis and antimalarial activity in vitro of new heterobimetallic complexes:  Rh and Au derivatives of chloroquine and a series of ferrocenyl-4-amino-7chloroquinolines.  M. A. L. Blackie, P. Beagley, K. Chibale, C. Clarkson, A. T. Hutton, J. R. Moss* and P. J. Smith. J. Organomet. Chem. 2003, 688, 144-152.   JIF =2.53

[26]      Synthesis of totarol amino alcohol derivatives and their antiplasmodial activity and cytotoxicity.  C. Clarkson, C. C. Musonda, K. Chibale*, W. E. Campbell and P. J. Smith.  Bioorg. Med. Chem, 2003, 11, 4417-4422.    JIF =3.04

[27]      Unprecedented observation of sulfonamides in the transesterification of N-unsubstituted carbamates with sulfonly chlorides.  J. Dauvergne, K. Wellington and K. Chibale*. Tetrahedron Lett., 2004, 45, 43-47  JIF =2.50

[28]      Application of combinatorial and parallel synthesis methodologies to antiparasite drug discovery, C. C. Musonda and K. Chibale*. Curr. Med. Chem. 2004, 11, 2519-2533.   JIF =5.38

[29]      Synthesis and Structure Activity Relationships of Parasiticidal Thiosemicarbazone Cysteine Protease Inhibitors against P.falciparum, T. brucei and T. cruzi.  D. Greenbaum*, Z. Mackey, E. Hansell, P. Doyle, J. Gut, C. R. Caffrey, J. Lehman, P. J. Rosenthal, J. H. McKerrow, and K. Chibale*.  J. Med. Chem. 2004, 47, 3212-3219.   JIF =5.17

[30]      Application of Multi-Component Reactions to Antimalarial Drug Discovery. Part 1.  Parallel Synthesis and Antiplasmodial Activity of New 4-Aminoquinoline Ugi Adducts. C. C. Musonda, D. Taylor, J. Lehman, J. Gut, P. J. Rosenthal and K. Chibale*. Bioorg. Med. Chem. Letts., 2004, 14, 3901-3905.  JIF =2.59

[31]      The new permeability pathways: targets and selective routes for the development of new antimalarial agents. H. M. Staines*, J. C. Ellory and K. Chibale. Combinatorial Chemistry and High Throughput Screening  2005, 8, 81-88.   JIF =2.24

[32]      Design, synthesis and antiplasmodial evaluation in vitro of new 4-aminoquinoline isatin derivatives.  I. Chiyanzu, C. Clarkson, P. J. Smith, J. Lehman, J. Gut. P. J. Rosenthal and K. Chibale*. Bioorg. Med. Chem., 2005, 13, 3249-3261.   JIF =3.04

[33]      Exploiting a basic chemosensitizing pharmacophore hypothesis. Part 1: synthesis and biological evaluation of novel arylbromide and bicyclic chemosensitizers against drug-resistant malaria parasites F. Chouteau, D. Ramanitrahasimbola, P. Rasoanaivo*and K. Chibale*. Bioorg. Med. Chem. Letts., 2005, 15, 3024-3028.  JIF =2.59

[34]      Reversal of chloroquine resistance in Plasmodium falciparum by 9H-xanthene derivatives. C.-P. Wu, D. A. van Schalkwyk, D. Taylor, P. J. Smith and K. Chibale*. International Journal of Antimicrobial Agents 2005, 26, 170-175   JIF =2.78

[35]      Economic drug discovery and rational medicinal chemistry for tropical diseases. K. Chibale*. Pure & Applied Chemistry 2005, 77, 1957-1964.  JIF =2.75

[36]      Arylpiperazines displaying preferential potency against chloroquine-resistant strains of the malaria parasite Plasmodium falciparum.  C.-A. Molyneaux, M. Krugliak, H. Ginsburg, and K. Chibale* Biochemical Pharmacology. 2005, 71, 61-68.  JIF =4.07

[37]     Inhibitors of the trypanosome alternative oxidase reduce parasite growth in culture.  RD Ott, K Chibale, S Anderson, A Chipeleme, M Chaudhuri, N Colowick, and G C Hill.  Faseb J.   2006  20 A938-A938   JIF =7.09

[38]      Novel Ketomethylene Inhibitors of Angiotensin-I Converting Enzyme (ACE): Inhibition and Molecular Modelling.  P. Redelinghuys, A. T. Nchinda, K. Chibale and E. D. Sturrock*.  Biological Chemistry, 2006, 387, 461-466.   JIF =2.91

[39]      Novel approaches to antimalarial drug discovery.  C. Biot*, and K. Chibale*. Infectious Disorders- Drug Targets-, 2006, 6, 173-204.  JIF = 4.82

[40]      Application of Multi-Component Reactions to Antimalarial Drug Discovery. Part 2.  New Antiplasmodial and Antitrypanosomal 4- Aminoquinoline γ– and δ Lactams via a “Catch and Release” Protocol.  C. C. Musonda, J. Gut, P. J. Rosenthal V. Yardley, R. C. Carvalho de Souza and K. Chibale*. Bioorg. Med. Chem.  2006, 14, 5605-5615.   JIF =3.04

[41]      Dual-Acting Diamine Antiplasmodial and Chloroquine Resistance Modulating Agents.  S. Yeh, P. J. Smith and K. Chibale*  Biochemical Pharmacology 2006, 72, 156-165.   JIF =4.07

[42]      Synthesis of Novel Keto-ACE Analogues as Domain-Selective Angiotensin-I Converting Enzyme Inhibitors A. T. Nchinda, K. Chibale, P. Redelinghuys, and E. D. Sturrock*. Bioorg. Med. Chem Lett.  2006, 16, 4612-4615.   JIF =2.59

[43]      Synthesis and Molecular Modeling of a Lisinopril-Tryptophan Analogue Inhibitor of Angiotensin I-Converting Enzyme.  A. T. Nchinda, K. Chibale, P. Redelinghuys, and E. D. Sturrock*. Bioorg. Med. Chem Lett.  2006, 16, 4616-4619.  JIF =2.59

[44]      Novel inhibitors of the trypanosome alternative oxidase inhibit Trypanosoma brucei brucei growth and respiration.  R. Ott, K. Chibale, S. Anderson, A. Chipeleme, M. Chaudhuri, A. Guerrah, N. Colowick, and G. C. Hill*.  Acta Tropica 2006, 100, 172-184.  JIF =2.44

[45]      Synthesis and Biological Evaluation of Phenolic Mannich Bases of Benzaldehyde and (thio) semicarbazone derivatives Against the Cystein Protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum.  A. Chipeleme, J. Gut, P. J. Rosenthaland K.  Chibale*. Bioorg. Med. Chem.  2007, 15, 273-282.  JIF =3.04

[46]      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.   JIF =1.84

[47]      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. Chouteau and K. Chibale. Phytochemistry 2007, 68, 1200-1205.   JIF =3.19

[48]      Application of Multicomponent Reactions to Antimalarial Drug Discovery. Part 3: Discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro.  C.C. Musonda, S. Little, V. Yardley and K. Chibale*. Bioorg. Med. Chem Lett.  2007, 17, 4733-4736.  JIF =2.59

[49]      Metallocene-based antimalarials: An exploration into the influence of the ferrocenyl moiety on in vitro antimalarial activity in chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum.  M.A.L. Blackie, P. Beagley, S. L. Croft, H. Kendrick, J. R. Moss and K. Chibale*. Bioorg. Med. Chem.  2007, 15, 6510-6516.    JIF =3.04

[50]      Synthesis of new 7-chloroquinolinyl thioureas and their biological investigation as potential anti-malarial and anticancer agents. A. Mahajan, S. Yeh, M. Nell, C E J van Rensburg and K. Chibale*. Bioorg. Med. Chem Lett.  2007, 17, 5683-5685.  JIF =2.59

[51]      Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues. C. Biot,* B. Pradines, M-H. Sergeant, J. Gut, P. J. Rosenthal and K. Chibale. Bioorg. Med. Chem Lett.  2007, 17, 6434-6438   JIF =2.59

[52]      Chemoselectivity and unusual internal acetal formation in the synthesis of a glycosidation precursor. A. T. Stevens, J. R. Bull and K. Chibale*.  Synlett  2007, 3175-3179.   JIF =2.61

[53]      Effect of varying the anionic component of a copper (I) catalyst on homologation of arylacetylenes to allenes by the Mannich reaction. V. Kumar, A. Chipeleme and K. Chibale*. Eur. J. Org. Chem.  2008, 43-46.   JIF =3.07

[54]      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.  JIF =3.76

[55]      Meclonazepam Analogues as Potential New Antihelmintic Agents. A. Mahajan, V. Kumar, N. R. N. Mansour, Q. Bickle and K. Chibale*. Bioorg. Med. Chem Lett.  2008, 18, 2333-2336   JIF =2.59

[56]      Metallocene Antimalarials: The Continuing Quest. M. A. L. Blackie and K. Chibale*. Metal-Based Drugs, 2008, 2008, 495123 doi:10.1155/2008/495123 JIF =Unknown

[57]      Inhibition of Trypanothione Reductase and Glutathione Reductase by Ferrocenic 4-Aminoquinoline Ureas. M. A. L. Blackie, A. Saravanamuthu, A. H. Fairlamb and K. Chibale*. Arkivoc, 2008, (vi), 52-60   JIF =1.21

[58]      Synthesis, antimalarial and cytotoxic evaluation of reversed chloroquines based on the 3,4-dihydropyrimidi-2(1H)-one scaffold. N. October, N. D. Watermeyer, V. Yardley, T. J. Egan, K. Ncokazi and K. Chibale*. ChemMedChem.  2008, 3, 1649-1653.   JIF =3.25

[59]      Antiplasmodial, b-haematin inhibition, antitrypanosomal and cytotoxic activity in vitro of novel 4-aminoquinoline 2-imidazolines. C.C. Musonda, V.Yardley, R. C. Carvalho de Souza, K. Ncokazi,T. J. Egan and K. Chibale*.  Org. Biomol. Chem., 2008, 6, 4446 – 4451   JIF =3.76

[60]      Synthetic Medicinal Chemistry of Antimalarial Natural Products. V. Kumar, A. Mahajan, and K. Chibale*. Bioorg. Med. Chem.  2009, 17, 2236-2275.  JIF = 3.04 Paper ranked in the top ten of the most popular/most cited articles for 2009-2010 academic year in this journal

[61]      Novel web-based tools combining chemistry informatics, biology and social networks for drug discovery. M. Hohman, K. Gregory, K. Chibale, P.J. Smith, S. Ekins and B. Bunin*. Drug Discovery Today, 2009,14, 261-70.   JIF =7.37

[62]      Synthesis of novel anti-2-alkoxy-3-amino-3-arylpropan-1-ols and cis-5-alkoxy-4aryl-1,3-oxazinanes with antimalarial activity. M. D’hooghe, P. J. Smith, S. Dekeukeleire, K. Mollet, K. Chibale and N. De Kimpe* J. Med. Chem.  2009, 52, 4058-4062.   JIF =5.17

[63]      Cycloaddition and One-Carbon Homologation Studies in the Synthesis of Advanced Iridoid Precursors. A. T. Stevens, M. R. Caira, J. R. Bull, and K. Chibale* Org. Biomol. Chem., 2009, 7, 3527- 3536.   JIF =3.76

[64]      Pharmacologically relevant bifunctional compounds containing chloroquinoline and dihydropyrimidone moieties; syntheses and crystal structures of a target molecule and selected intermediates. N. D. Watermeyer, K. Chibale* and M.R. Caira*.  J. Chem. Crystallography. 2009, 39, (10), 753-760   JIF =0.63

[65]      A New and Simple Synthesis of Sulfonyl Ureas from Sulfonamides and N-Alkyl-1,2,4-dithiazolidine-3,5-diones. R.K. Gessner and K. Chibale*.  Synlett. 2009, 17, 2839-2843    JIF =2.61

[66]      Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo. M.A.L. Blackie, V. Yardley, and  K. Chibale*. Bioorg. Med. Chem. Lett.  2010, 20, 1078-1080.  JIF =2.59

[67]      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.   JIF =2.59. Article recognised as a “Top-25 Most Cited Article 2010-2011″.

[68]      Gold (I) Derived Thiosemicarbazone Complexes with rare halogen-halogen interaction-Reduction of [Au(damp-C1,N)Cl2], S. Khanye; N. B. Bathori, G. S. Smith, and  K. Chibale*. Dalton Transactions, 2010, 39 (10), 2697 – 2700.     JIF =3.93

[69]      Comparison of the Antiplasmodial and Falcipain-2 Inhibitory Activity of β-Amino Alcohol Thiolactone-Chalcone and Isatin-Chalcone Hybrids. R.H. Hans, J. Gut, P.J. Rosenthal, and K. Chibale* Bioorg. Med. Chem. Lett.  2010, 20, 2234-2237.  JIF =2.59

[70]      Chloroquine resistance: proposed mechanisms and countermeasures. E. M. Guantai and K. Chibale*.  Current Drug Delivery. 2010, 7, 312-323 JIF = 1.5

[71]       CRIMALDDI: a co-ordinated, rational, and integrated effort to set logical priorities in antimalarial drug discovery initiatives. I. C Boulton*, S. Nwaka, I. Bathurst, M. Lanzer, D. Taramelli, H. Vial, C. Doerig, S. M. N. Efange, K. Chibale & S.A. Ward* Malaria Journal.  2010, 9, 202   JIF =3.49

[72]      Thiosemicarbazone Salicylaldiminato Palladium(II)-Catalyzed Mizoroki-Heck Reactions. G. Xie, P. Chellan, J. Mao*, K. Chibale, G. S. Smith* Advanced Synthesis & Catalysis 2010, 352, 1641-1647. JIF =5.47

[73]      Synthesis, structures and in vitro biological screening of palladium(II) complexes of functionalised salicylaldimine thiosemicarbazones as antimalarial and anticancer agents.  P. Chellan, N. Shunmoogam-Gounden, D.T. Hendricks, J.Gut, P. J. Rosenthal, C. Lategan, P. J. Smith, K. Chibale, G.S. Smith*.  Eur.J. Inorg. Chem.  2010, 3520-3528.   JIF =3.10

[74]      Cyclopalladated Complexes Containing Tridentate Thiosemicarbazone Ligands of Biological Significance: Synthesis, Structure and Antimalarial activity.  P. Chellan, S. Nasser, K. Chibale, G. S. Smith*.  Journal of Organometallic Chemistry.  2010, 695, 2225-2232.   JIF =2.53

[75]      Synthesis and in vitro evaluation of gold(I) thiosemicarbazone complexes for antimalarial activity.  S.D. Khanye, G. Smith, J. Gut, P. J. Rosenthal and K. Chibale*.  Journal of Inorganic Biochemistry  2010, 104, 1079-1083.  JIF =3.71

[76]      Novel Tetracyclic Structures from the Synthesis of Thiolactone-Isatin Hybrids.  R. H. Hans, H. Su and K. Chibale*.  Belstein Journal of Organic Chemistry  2010, 6,(78), 1-7 ( doi: 10.3762/bjoc.6.78) JIF=1.26

[77]      Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds.  E. M. Guantai, K. Ncokazi a, T. J. Egan, J. Gut, P. J. Rosenthal, P. J. Smith, and K. Chibale*.  Bioorg. Med. Chem.  2010, 18, 8243-8256.  JIF =3.04

[78]    Synthesis of 2-(aminomethyl)aziridines and their microwave-assisted ring opening to 1,2,3-triaminopropanes as novel antimalarial pharmacophores. M. D’hooghe,*, S. Kenis, K. Vervisch, C. Lategan , P. J. Smith, K. Chibale, N. De Kimpe* Eur. J. Med. Chem.  2011, 46, 579-587 JIF =3.36

[79]      Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents. R.H. Hans, I. J. F. Wiid, P. D. Van Helden, B. Wan, S.G. Franzblau, J. Gut, P.J. Rosenthal, and K. Chibale* Bioorg. Med. Chem. Lett.  2011, 21, 2055-2058. JIF =2.59

[80]      How can natural products serve as a viable source of lead compounds for the development of new/novel antimalarials? E. M. Guantai and K. Chibale* Malaria Journal  2011, 10(Suppl 1):S2 (15 March 2011). JIF =3.49

[81]      Extracting molecular information from African natural products to facilitate unique African-led drug discovery efforts. E. M. Guantai. C. M. Masimirembwa, and K. Chibale* Future Medicinal Chemistry.  2011,3(3) 257-261 JIF = 1.4

[82]    Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity. K. Singh, K. Singh, B. Wan, S. Franzblau, K. Chibale and J. Balzarini Eur. J. Med. Chem.  2011, 46, 2290-2294.  JIF =3.36

[83]      The state of the art in anti-malarial drug discovery and development.  J. Burrows, K. Chibale and T.N.C. Wells.  Current Topics in Medicinal Chemistry 2011, 11 (10), 1226-1254. JIF =4.31

[84]      Antiplasmodial and antitumour activity of artemisinin analogs derived via the aza-Michael addition reaction. T.-S Feng; E. M. Guantai, M. J. Nell; C.E.J van Rensburg; H. C. Hoppe, and K. Chibale* Bioorg. Med. Chem. Lett.  2011, 21, 2882-2886. JIF =2.59

[85]      Synthesis and in vitro antitubercular activity of ferrocene-based hydrazones.  A. Mahajan, L. Kremer, S. Louw, Y. Guéradel, K. Chibale, and C. Biot* Bioorg. Med. Chem. Lett.  2011, 21, 10, 2866-2868. JIF =2.59

[86]     Linear free energy relationships predict coordination and π-stacking interactions of small molecules with ferriprotoporphyrin IX.  D. Kuter, K. Chibale, and T. J. Egan*.  Journal of Inorganic Biochemistry  2011, 105, 684-692.  JIF =3.71

[87]     Molecular Structure of an Unexpected Binuclear Salicylaldimine Semicarbazone Palladium(II) Complex. P. Chellan, K. Chibale and G. S. Smith*.  J Chem Crystallography, 2011, 41, 747-750 JIF =0.63

[88]      Enone- and chalcone-chloroquinoline hybrid analogs: In silico-guided design, synthesis, antiplasmodial activity, in vitro metabolism and mechanistic studies. E. M. Guantai, K. Ncokazi, T. J. Egan, J. Gut, P. J. Rosenthal, R. Bhampidipati, A. Kopinathan, P. J. Smith and K. Chibale*  J. Med. Chem.  2011, 54, 3637–3649.   JIF =5.17

[89]      Effects of highly active novel artemisinin-chloroquinoline hybrid compounds on beta-hematin formation, parasite morphology and endocytosis in Plasmodium falciparum. T.-S Feng, E.M. Guantai, M. Nell, C.E.J van Rensburg, K. Ncokazi, T. J. Egan, H. C. Hoppe* and K. Chibale* Biochemical Pharmacology 2011, 82, 236–247 JIF (2011) = 4.705

[90]      Antimalarial Pyrido[1,2-a]benzimidazoles. A.J. Ndakala, R.K. Gessner, P.W. Gitari,N. October, K.L. White, A. Hudson,F. Fakorede,D.M. Shackleford,  M. Kaiser, C. Yeates, S.A. Charman, and K. Chibale*  J. Med. Chem.  2011, 54, 4581–4589 .   JIF =5.17

[91]      Antiplasmodial and Cytotoxicity Evaluation of 3-functionalized 2-Azetidinone derivatives. P. Singh,S. Sachdeva,R. Raj, Vipan Kumar,* M.P. Mahajan, S. Nasser, L. Vivas, J. Gut, P.J. Rosenthal, T.-S. Feng, and  K. Chibale Bioorg. Med. Chem. Lett.  2011, 21, 4561–4563 JIF =2.59

[92]      Drug repositioning in the treatment of malaria and tuberculosis. A. Nzila*, Z. Ma, and K. Chibale Future Medicinal Chemistry.  2011,3(11) 1413-1426 JIF = 1.4

[93]      Ferrocenylthiosemicarbazones Conjugated to a Poly(propyleneimine) Dendrimer Scaffold: Synthesis and In Vitro Antimalarial Activity S.D. Khanye, K. Chibale*, G. S. Smith*.  Journal of Organometallic Chemistry.  2011, 696, 3296-3300.   JIF =2.53

[94]      Synthesis and in vitro antimalarial and antitubercular activity of gold(III) complexes containing thiosemicarbazone ligands S.D. Khanye, B. Wan, S.G. Franzblau, J.Gut, P.J. Rosenthal, G.S. Smith*, K. Chibale,* Journal of Organometallic Chemistry.  2011, 696, 3392-3396.   JIF =2.53

[95]      Synthesis and in vitro evaluation of palladium(II) salicylaldiminato thiosemicarbazone complexes against Trichomonas vaginalis.  P. Chellan, T. Stringer, A. Shokar, P.J. Dornbush, G. Vazquez-Anaya, L.A. Wrischnik, K.M. Land, K. Chibale and G.S. Smith*.  Journal of Inorganic Biochemistry  2011, 105, 1562-1568.  JIF =3.71

[96]      Quinoline Antimalarials Containing a Dibemethin Group are Active against Chloroquine Resistant P. falciparum and Inhibit Chloroquine Transport via the Plasmodium falciparum Chloroquine-Resistance Transporter (PfCRT) V.K Zishiri, M.C. Joshi, R. Hunter, K. Chibale, P.J. Smith, R.L. Summers, R.E. Martinand T.J. Egan*  J. Med. Chem.  2011, 54, 6956–6968  JIF =5.17

[97]      The Significance of the Cá Substituent in the Selective Inhibition of Matrix Metalloproteinase 1 and 9. R. Domingo, K. Chibale and E. D. Sturrock* Biological Chemistry, 2011, 392, 1003–1010 JIF =2.91

[98]      Novel Orally Active Antimalarial Thiazoles. D. G. Cabrera, F. Douelle, T.-S Feng, A.T. Nchinda, Y. Younis, K. L. White,  Q. Wu,E. Ryan, J. N. Burrows,D. Waterson, M. J. Witty,S. Wittlin,S. A. Charman and K. Chibale*  J. Med. Chem.  2011, 54, 7713–7719. JIF =5.17

[99]      Synthesis of 2-amino-3-arylpropan-1-ols and 1-(2,3-diaminopropyl)-1,2,3-triazoles and evaluation of their antimalarial activity M. D’hooghe*, S. Vandekerckhove1, K. Mollet, K. Vervisch1, S. Dekeukeleire, L. Lehoucq, C. Lategan, P. J. Smith, K. Chibale and N. De Kimpe* Beilstein J. Org. Chem. 2011, 7, 1745–1752 JIF (2011) = 2.517

[100]    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.  JIF =3.04

[101]   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 JIF= 2.872

[102]   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 JIF= 2.527

[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. JIF =5.207

[104]   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, JIF= 5.28

[105]   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. JIF =3.36

[106]    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 JIF = 2.7

[107]    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 JIF =2.91

[108]    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. JIF = 3.89

[109]    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  JIF =2.59

[110]    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 JIF =3.04

[111]    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  JIF =3.04

[112]    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 JIF = 3.571

[113]   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. JIF =3.36

[114]    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 JIF = 1.4

[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. JIF = 1.4

[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. JIF =5.207

[117]    Synthesis and antiplasmodial evaluation of novel (4-aminobutyloxy)quinolines. S. Vandekerckhove, C. Müller, D. Vogt, C. Lategan, P. J. Smith, K. Chibale, N. De Kimpe, M. D’hooghe Bioorg. Med. Chem. Lett.  2013, 23, 318-322 JIF = 2.59

[118]    Cyclometallated Pd(II) thiosemicarbazone complexes: new catalyst precursors for Suzuki-coupling reactions H. Yan, P. Chellan, T. Li, Jincheng Mao*, K. Chibale, G. S. Smith*   Tetrahedron Letts 2013, 54, 154-157. JIF = 2.683

[119]   Synthesis, antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives. M. Tukulula, R.-K.Sharma,M. Meurillon, A. Mahajan, K. Naran, D. Warner, J. Huang, B. Mekonnen, and K. Chibale,* ACS Med. Chem. Lett. 2013, 4, 128−131. JIF = 3.355

[120]    Synthesis of 2-aminomethyl-4-phenyl-1-azabicyclo[2.2.1]heptanes via LiAlH4-induced reductive cyclization of  2-(4-chloro-2-cyano-2-phenylbutyl)aziridines and evaluation of their antimalarial activity. M. D’hooghe *, K. Vervisch, K. W. Törnroos, T. Verhaeghe, T. Desmet, C. Lategan, P.J. Smith, K. Chibale, N. De Kimpe *  Bioorg. Med. Chem. Lett.  2013, 23, 1507–1510 JIF = 2.59

[121]    Synthesis, Characterization and Pharmacological Evaluation of Silicon-Containing Aminoquinoline Organometallic Complexes as Antiplasmodial, Antitumor and Antimycobacterial Agents . Y. Li, C. de Kock, P.J. Smith, H. Guzgay, D.T. Hendricks, K. Naran, V. Mizrahi, D. F. Warner, K. Chibale* and G. S. Smith*. Organometallics 2013, 32, 141−150. JIF = 3.89

[122]    The synthesis and antiparasitic activity of aryl and ferrocenyl-derived thiosemicarbazone ruthenium(II)–arene complexes. M. Adams, Y. Li, H. Khot, C. De Kock, P. J. Smith, K. Land, K. Chibale and G. S. Smith*. Dalton Trans., 2013, 42 (13), 4677 – 4685 JIF =3.93

[123]   Recent Developments in Rationally Designed Multitarget Antiprotozoan Agents. P. M. Njogu and K. Chibale*. Curr. Med. Chem., 2013, 20(13), 1715-1742 .   JIF = 5.38  

[124]    Synthesis and antiplasmodial evaluation of aziridine-(iso)quinoline hybrids and their ring-opening products.  S. Vandekerckhove, S. De Moor, D. Segers, C. de Kock, P. J. Smith, K. Chibale, N. De Kimpe* and M. D’hooghe* Med. Chem. Commun., 2013, 4, 724–730 JIF =2.800

[125]    In silico Comparison of Antimycobacterial Natural Products with Known Antituberculosis Drugs.  M. Espinoza-Moraga, N. Njuguna, G. Mugumbate, J. Caballero and K. Chibale* J. Chem. Inf. Model. 2013, 53, 649−660.   JIF = 4.675

[126]    Synthesis, characterization and antiplasmodial evaluation of cyclopalladated thiosemicarbazone complexes. M. Adams, C. de Kock, P.J. Smith, K. Chibaleand G. S. Smith,* Journal of Organometallic Chemistry.  2013, 736, 19−26 JIF = 2.53

[127]    Structure-activity relationships for ferriprotoporphyrin IX association and <beta>-hematin inhibition by 4-aminoquinolines using experimental and ab initio methods. S. Nsumiwa, D. Kuter, S. Wittlin, K. Chibale, T.J. Egan* *Bioorg. Med. Chem.  2013, 21, 3738-3748 JIF =3.04

[128]   Synthesis of 4-aminoquinoline–pyrimidine hybrids as potent antimalarials and their mode of action studies. K. Singh,* H. Kaur, K. Chibale, and J. Balzarini,  Eur. J. Med. Chem.  2013, 66, 314-323. JIF =3.36

[129]    Synthesis, Antiplasmodial Activity and β-hematin Inhibition of Hydroxypyridone -Chloroquine Hybrids. A.W. Andayi, T. J. Egan,J. Gut, P.J. Rosenthal, and K. Chibale,* ACS Med. Chem. Lett. 2013, 4, 642−646  JIF = 3.355

[130]    Design, Synthesis and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-Phenylisoserine. P. Njogu,J. Gut, P.J. Rosenthal, and K. Chibale,* ACS Med. Chem. Lett. 2013, 4, 637−641 JIF = 3.355

[131]    Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential     antimalarial agents.  M. Tukulula, M. Njoroge, G. C. Mugumbate, J. Gut, P.J. Rosenthal, S. Barteau, J. Streckfuss, O. Heudi,  J. Kameni-Tcheudji, and K. Chibale* Bioorg. Med. Chem.  2013, 21, 4904–4913  JIF =3.04

 [132]   Cell-based Medicinal Chemistry Optimization of High Throughput Screening (HTS) Hits for Orally Active Antimalarials-Part 2: Hits from SoftFocus Kinase and other Libraries. Y. Younis, L. J. Street, D. Waterson, M.J. Witty, and K. Chibale.* J. Med. Chem. 2013, 56, 7750−7754  JIF =5.207

[133]    Heterobimetallic ferrocenylthiosemicarbazone palladium(II) complexes: Synthesis, electrochemistry and antiplasmodial evaluation.  M. Adams, C. de Kock, P. J. Smith, P. Malatji, A.T. Hutton, K. Chibaleand G. S. Smith.* Journal of Organometallic Chemistry 739 (2013) 15-20 JIF =2.53

[134]    Di- and Trinuclear Ruthenium, Rhodium, and Iridium-Functionalized Pyridyl Aromatic Ethers: A New Class of Antiparasitic Agents. P. Chellan, K.M. Land, A. Shokar, A. Au, S. Hwan An, D. Taylor, P.J. Smith, K. Chibale and G.S. Smith* Organometallics 2013, 32, 4793−4804. JIF = 3.89

[135]    3-Hydroxyisoflavanones from the stem bark of Dalbergia melanoxylon: Isolation, antimycobacterial evaluation and molecular docking studies. P. Mutai, M. Heydenreich, G. Thoithi, G. Mugumbateb, K. Chibale and A. Yenesew* Phytochemistry Letters  2013, 6, 671−675. JIF = 1.353

[136]    Structure-Activity-Relationship Studies Around the 2-Amino Group and Pyridine Core of Antimalarial 3,5-Diarylaminopyridines Lead to a Novel Series of Pyrazine Analogues with Oral in vivo Activity. Y. Younis, F. Douelle,D. G. Cabrera, C. Le Manach, A.T. Nchinda, T. Paquet, L.J. Street, K. L. White,K. M. Zabiulla, J.T. Joseph, S. Bashyam, D. Waterson,M.J. Witty,S. Wittlin,S.A. Charman, and K. Chibale*   J. Med. Chem. 2013, 56, 8860−8871. JIF =5.207

[137]    CRIMALDDI: platform technologies and novel anti-malarial drug targets. H. Vial, D. Taramelli, I.C. Boulton, S. A. Ward*, C. Doerig and K. Chibale  Malaria Journal  2013, 12, 396. JIF =3.40

[138] Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum. C. Le Manach, C. Scheurer, S. Sax, S. Schleiferböck, D. G. Cabrera, Y. Younis, T. Paquet, L. Street, P. J. Smith, X. Ding, D. Waterson, M. J.Witty, D. Leroy, K. Chibale and S. Wittlin*. Malaria Journal 2013, 12, 424 JIF = 3.40

[139]    Novel anti-Plasmodial hits identified by virtual screening of the ZINC database. G. Mugumbate, A.S. Newton, P.J. Rosenthal, J.Gut, R. Moreira, K. Chibale*, and R.C. Guedes*  J Comput Aided Mol Des 2013, 27, 859–871  JIF = 3.172

[140]   Synthesis, in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds. M. Tukulula, M. Njoroge, E.T. Abay, G. Mugumbate, L. Wiesner, D. Taylor, L. Gibhard, J. Norman, K.J. Swart, J. Gut, P.J. Rosenthal, S. Barteau, J. Streckfuss, J. Kameni-Tcheudji, K. Chibale.* ACS Med. Chem. Lett. 2013, 4, 1198−1202. JIF = 3.355

[141]    Anticancer properties of distinct antimalaria drug classes. R. H. van Huijsduijne, R.K. Guy, K. Chibale, R.K. Haynes, I. Peitz, G. Kelter, M. A. Phillips, J.L. Vennerstrom, Y. Yuthavong, and T.N. C. Wells*. PLoS One., 2013, 8(12) e82962. doi:10.1371/journal.pone.0082962 JIF =4.09

[142]   Drug metabolite generation using a laboratory evolved NADPH  independent cytochrome P450: application of in vitro and in silico approaches. N. T. L. Chigorimbo-Murefu, S. Louw, M. Njoroge, G. Mugumbate and K. Chibale.* Drug Metabolism Letters.  2013, 21, 68-77. JIF =4.90

[143]    Fragment-based design for the development of N-domain-selective angiotensin-1-converting enzyme inhibitors. R.G. Douglas, R.K. Sharma, G. Masuyer, L. Lubbe, I. Zamora, K.R. Acharya*, K. Chibale* and E.D Sturrock* Clinical Science 2014, 126, 305−313. JIF = 4.859

[144]    Synthesis and evaluation of new polynuclear organometallic Ru(II), Rh(III) and Ir(III) pyridyl ester complexes as in vitro antiparasitic and antitumor agents. P. Chellan, K.M. Land, A.Shokar, A. Au, S. H. An, D. Taylor, P. J. Smith,T. Riedel, P. J. Dyson, K. Chibale and G. S. Smith* Dalton Trans., 2014, 43(2), 513 – 526  JIF =3.93

[145]    Synthesis and biological evaluation of 2-aminothiazole derivatives as antimycobacterial and antiplasmodial agents. F. Mjambili, M. Njoroge, K. Naran, C. De Kock, P.J. Smith, V. Mizrahi, D. Warner, and K. Chibale*.  Bioorg. Med. Chem. Lett.  2014, 24, 560–564  JIF = 2.59

[146]    Synthesis of Metergoline analogues and their evaluation as antiplasmodial agents. K. Singh, G. Kaur, F. Mjambili, P. J. Smith and K. Chibale*. Med. Chem. Commun., 2014, 5 (2), 165 – 170.  JIF = 2.80

[147]    Synthesis of halogenated 4-quinolones and evaluation of their antiplasmodial activity. S. Vandekerckhove, T. Desmet, H. G. Tran, C. de Kock, P.J. Smith, K. Chibale and M. D’hooghe* Bioorg. Med. Chem. Lett.  2014, 24, 1214–1217  JIF = 2.59

[148]    The development and validation of an LC-MS/MS method for the determination of a new anti-malarial compound (TK900D) in human whole blood and its application to pharmacokinetic studies in mice. E. T. Abay, J.H. van der Westuizen, K.J. Swart, L. Gibhard, M. Tukulula , K. Chibale, L. Wiesner*.  Malaria Journal 2014, 13, 42. JIF =3.40

[149]   Quinoline–pyrimidine hybrids: Synthesis, antiplasmodial activity, SAR and mode of action studies. K. Singh*, H. Kaur; P. J. Smith, C. de Kock, K. Chibale, J. Balzarini J. Med. Chem. 2014, 57, 435−448. JIF =5.614

[150]    2,4-Diamino-thienopyrimidines as Orally Active Antimalarial Agents. D. G. Cabrera, C. Le Manach, F. Douelle, Y. Younis, T.-S. Feng, T. Paquet, A.T. Nchinda, L. J. Street, D. Taylor, C. de Kock, L. Wiesner, S. Duffy, K.L. White, K.M. Zabiulla, Y. Sambandan, S. Bashyam, D. Waterson, M.J. Witty,  S.A. Charman, V.M. Avery, S. Wittlin, and K. Chibale*. J. Med. Chem. 2014, 57, 1014-1022. JIF =5.614

[151]    Synthesis and synergistic antimycobacterial screening of chlorpromazine and its metabolites.  E.M. Kigondu, M. Njoroge, K. Singh, N. Njuguna, D. F. Warner, and K. Chibale*. Med. Chem. Commun., 2014, 5, 502–506 JIF = 2.80

[152]    Synthesis and medicinal chemistry of selected antitubercular natural products and natural product derivatives. A. Mahajan, R. Hans, K. Chibale, V.Kumar,* RSC Adv., 2014, 4, 15180–15215. JIF = 2.562 (partial)

[153]      Alternative solid-state forms of a potent antimalarial aminopyridine: X-ray crystallographic, thermal and solubility aspects. D.L. Cruickshank,Y.Younis, N.M. Njuguna, D.S. B. Ongarora, K. Chibale and Mino R. Caira* CrystEngComm. 2014, 16, 5781–5792 JIF = 3.879

[154]   Pharmacokinetic evaluation of lisinopril-tryptophan, a novel C-domain ACE inhibitor. P. Denti, S.-K. Sharp, W.L. Kröger, S. L. Schwager, A. Mahajan, M. Njoroge, L. Gibhard, I. Smit, K. Chibale, L. Wiesner, E. D. Sturrock*, N. Davies. European Journal of Pharmaceutical Sciences 2014, 56, 113–119  JIF = 3.418

[155]    Effects of a domain-selective ACE inhibitor in a mouse model of chronic angiotensin II-dependent Hypertension. D. Burger, T.L. Reudelhuber, A. Mahajan, K. Chibale, E.D. Sturrock, and R.M. Touyz*. Clinical Science 2014, 127, 57–63. JIF = 4.859

[156]    Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 1.  C. Le Manach, D. Gonzalez Cabrera, F. Douelle, A. T. Nchinda, Y. Younis, D. Taylor, L. Wiesner, K. White, E. Ryan, C. March, S. Duffy, V. Avery, D. Waterson, M. J. Witty, S. Wittlin; S. Charman, L. Street, and K. Chibale*. J. Med. Chem. 2014, 57, 2789-2798. JIF =5.614

[157]    Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.  Kawaljit Singh, Malkeet Kumar, Elumalai Pavadai, Krupa Naran, Digby F. Warner, Peter G. Ruminskiand Kelly Chibale  Bioorg. Med. Chem. Lett.  2014, 24, 2985–2990. JIF = 2.59

[158]    Kojic acid derived hydroxypyridinone-chloroquine hybrids: Synthesis, crystal structure, antiplasmodial activity and <beta>-haematin inhibition W. A. Andayi, T. J. Egan and Kelly Chibale* Bioorg. Med. Chem. Lett.  2014, 24, In press, accepted for publication. JIF = 2.59

[159]    Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.  E.M. Kigondu, A. Wasuna, D.F. Warner*, and K. Chibale*. Bioorg. Med. Chem.  2014, 22, In press, accepted for publication JIF =3.04

[160]    Recent Approaches to Chemical Discovery and Development Against Malaria and the Neglected Tropical Diseases Human African Trypanosomiasis and Schistosomiasis.  M. Njoroge, N. Njuguna, P. Mutai, D. Ongarora, P. Smith, and K. Chibale*. Chemical Reviews.  2014, 114, In press, accepted for publication JIF = 41.298

 

 


 

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