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Issue 33, 2015
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Polyamine quinoline rhodium complexes: synthesis and pharmacological evaluation as antiparasitic agents against Plasmodium falciparum and Trichomonas vaginalis

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Abstract

A series of mono- and bis-salicylaldimine ligands and their corresponding Rh(I) complexes were prepared. The compounds were characterised using standard spectroscopic techniques including NMR, IR spectroscopy and mass spectrometry. The salicylaldimine ligands and complexes were screened for antiparasitic activity against two strains of Plasmodium falciparum i.e. the NF54 CQ-sensitive and K1 CQ-resistant strain as well as against the G3 isolate of Trichomonas vaginalis. The monomeric salicylaldimine quinolines exhibited good activity against the NF54 strain and the dimeric salicylaldimine quinolines exhibited no cross resistance across the two strains. The binuclear 5-chloro Rh(I) complex displayed the best activity against the Trichomonas vaginalis parasite, possibly a consequence of its enhanced lipophilicity. The compounds were also screened for cytotoxicity in vitro against WHCO1 oesophageal cancer cells. The monomeric salicylaldimine quinolines exhibited high selectivity towards malaria parasites compared to cancer cells, while the dimeric compounds were less selective.

Graphical abstract: Polyamine quinoline rhodium complexes: synthesis and pharmacological evaluation as antiparasitic agents against Plasmodium falciparum and Trichomonas vaginalis

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Publication details

The article was received on 23 Jun 2015, accepted on 16 Jul 2015 and first published on 30 Jul 2015


Article type: Paper
DOI: 10.1039/C5DT02378E
Citation: Dalton Trans., 2015,44, 14906-14917
  • Open access: Creative Commons BY-NC license
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    Polyamine quinoline rhodium complexes: synthesis and pharmacological evaluation as antiparasitic agents against Plasmodium falciparum and Trichomonas vaginalis

    T. Stringer, D. Taylor, H. Guzgay, A. Shokar, A. Au, P. J. Smith, D. T. Hendricks, K. M. Land, T. J. Egan and G. S. Smith, Dalton Trans., 2015, 44, 14906
    DOI: 10.1039/C5DT02378E

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