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Refereed Journals

2017

[210] 4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group are Active against Drug Resistant <i>Plasmodium falciparum</i> and Exhibit Oral Activity in Mice"
Author(s): M. Joshi, J. Okombo, S. Nsumiwa, J. Ndove, D. Taylor, L. Wiesner, R. Hunter, K. Chibale, and T. Egan*J. Med. Chem. 2017, 60, 10245−10256
[209] Novel Anti-tubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure Activity Relationship and Target Identification Studies.  C. Wilson, R. Gessner, A. Moosa, R. Seldon, D. Warner, V. Mizrahi, C. Soares de Melo, S. Simelane, A. Nchinda, E. Abay, D. Taylor, M. Njoroge, C. Brunschwig, N. Lawrence, H. Boshoff, C.E. Barry, F. Sirgel, P. van Helden, C. J. Harris, R. Gordon, S. Ghidelli-Disse, H. Pflaumer, M. Boesche, G. Drewes, O. Sanz, G. Santos, M. J. Rebollo-Lopez, B. Urones, C. Selenski, M. Lafuente-Monasterio, M. Axtman, J. Lelièvre, L. Ballell, R. Mueller; L. Street, S. Ghorpade* and K. Chibale*J. Med. Chem. 2017, 60, 10118−10134
[208] Antimicrobial activity of organometallic isonicotinyl and pyrazinyl ferrocenyl-derived complexes. T. Stringer, R. Seldon N. Liu, D. F. Warner, Christina Tam, L. W. Cheng, K. M. Land, P.J. Smith, P.J. Smith, K. Chibale and G.S. Smith*, Dalton Trans., 2017, 46, 9875–9885
[207] Insights into Integrated Lead Generation and Target Identification in Malaria and Tuberculosis Drug Discovery J. Okombo and K. Chibale* Acc. Chem. Res. 2017, 50, 1606−1616.  DOI 10.1021/acs.accounts.6b00631
[206] Identification of steroid-like natural products as antiplasmodial agents by 2D and 3D similarity-based virtual screening. E. Pavadai,* G. Kaur, S. Wittlin and K. Chibale*. Med. Chem. Commun. 2017, 8, 1152–1157  Article featured on front cover of the journal issue and part of the themed collection

2017 Hot Articles in MedChemComm

[205] Antischistosomal Activity of Pyrido[1,2-a]benzimidazole Derivatives and Correlation with Inhibition of β-haematin Formation.  J. Okombo, K. Singh, G. Mayoka, F. Ndubi, L. Barnard, P. M. Njogu, M. Njoroge, L. Gibhard, C. Brunschwig, M. Vargas, J. Keiser, T. J. Egan and K. Chibale* ACS Infect. Dis. 2017, 3, 411−420
[204] Intestinal Transport Characteristics and Metabolism of C-Glucosyl Dihydrochalcone, Aspalathin.  S. Bowles*, E. Joubert, D. de Beer, J. Louw, C. Brunschwig, M. Njoroge, N. Lawrence, L. Wiesner, K. Chibale, and C. Muller. Molecules 2017, 22, 554
[203] Anti-malarial efficacy and parasite life cycle characterisation of the novel Plasmodium phosphatidylinositol 4-kinase inhibitor MMV390048T. Paquet, C. Le Manach, D. González Cabrera, Y. Younis, P. P. Henrich, T. S. Abraham, M. C.S. Lee, R. Basak, S. Ghidelli-Disse, M. José Lafuente-Monasterio, M. Bantscheff, A. Ruecker, A. M. Blagborough, S.E. Zakutansky, A.-M. Zeeman, K. L. White, D. M. Shackleford, J. Mannila, J. Morizzi, C. Scheurer, I. Angulo-Barturen, M. S. Martínez, S. Ferrer, L. M. Sanz, F. Javier Gamo, J. Reader, M. Botha,  K. J. Dechering, R. W. Sauerwein, A. Tungtaeng, P. Vanachayangkul, C. S. Lim, J. Burrows, M. J. Witty, K. C. Marsh, C. Bodenreider, R. Rochford, S.M. Solapure, M. B. Jiménez-Díaz, S. Wittlin, S. A. Charman, C. Donini, B. Campo, L.-M. Birkholtz, K. K. Hanson, G. Drewes, C. H.M. Kocken, M. J. Delves,  D. Leroy, D.A. Fidock, D. Waterson, L. J. Street, and K. Chibale*Sci. Transl. Med., 2017, 9 (Issue 387), eaad9735 DOI: 10.1126/scitranslmed.aad9735.  Published online on 26 Apr 2017
[202] Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.  P. Mutai, G. Breuzard, A. Pagano, D. Allegro, V. Peyrot*, and K. Chibale*  Bioorg. Med. Chem.  2017, 25, 1652–1665
[201] Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents.  R. De Vreese, C. de Kock, P.J. Smith, K. Chibale, and M. D'hooghe*  Future Med. Chem. 2017, 9(4), 357–364
[200] Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics and In Vivo Oral Efficacy in a Mouse Model. K. Singh, J. Okombo, C. Brunschwig, F. Ndubi, L. Barnard, C. Wilkinson, P. M. Njogu, M. Njoroge, L. Laing, M. Machado, M. Prudêncio, J. Reader, M. Botha, S. Nondaba, L.-M. Birkholtz, S. Lauterbach, A. Churchyard, T. L. Coetzer, J. N. Burrows, C. Yeates, P. Denti, L. Wiesner, T. J. Egan, S. Wittlin, and K. Chibale*.  J. Med. Chem. 2017, 60, 1432−1448 
[199] The Role of Natural Products in Drug Discovery and Development against Neglected Tropical Diseases. P. M. Cheuka, G. Mayoka, P. Mutai and K. Chibale*  Molecules 2017, 22(1), 58;
[198] Synthesis and biological characterisation of ester and amide derivatives of Fusidic acid as antiplasmodial agents.  M. Espinoza, K. Singh, M. Njoroge, G. Kaur, J. Okombo, C. De Kock, P.J. Smith, S. Wittlin and K. Chibale*.  Bioorg. Med. Chem. Lett.  2017, 27, 658-661  
[197] Evaluation of Ferrocenyl-Containing Benzothiazoles as Potential Antiplasmodial Agents.  M. Adams, C. de Kock, P. J. Smith, K. Chibale, and G. S. Smith*. Eur. J. Inorg. Chem. 2017, 242–246.