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Papers in refereed journals

2011

[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.
[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

[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.

[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. Martin and T.J. Egan* J. Med. Chem. 2011, 54, 6956-6968.

[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.

[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.

[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.

[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.

[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.

[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.

[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.

[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.

[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.

[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.

[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)

[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.

[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.

[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.

[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.

[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).

[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.

[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.