NDLI: Improved antiparasitic activity by incorporation of organosilane entities into half-sandwich ruthenium(II) and rhodium(III) thiosemicarbazone complexes

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Smith, Peter J. Stringer, Tameryn Adams, Muneebah Meyer, Mervin Burgoyne, Andrew R. Hsiao, Allyson Smith, Gregory S. Land, Kirkwood M. Chibale, Kelly De Kock, Carmen Liu, Nicole Wiesner, Lubbe Hopper, Melissa
Description	Author Affiliation: Adams M ( Department of Chemistry, University of Cape Town, Rondebosch 7701, Cape Town, South Africa. Gregory.Smith@uct.ac.za.)
Abstract	A series of ferrocenyl- and aryl-functionalised organosilane thiosemicarbazone compounds was obtained via a nucleophilic substitution reaction with an amine-terminated organosilane. The thiosemicarbazone (TSC) ligands were further reacted with either a ruthenium dimer $[(η^{6-i}PrC_{6}H_{4}Me)Ru(μ-Cl)Cl]_{2}$ or a rhodium dimer $[(Cp*)Rh(μ-Cl)Cl]_{2}$ to yield a series of cationic mono- and binuclear complexes. The thiosemicarbazone ligands, as well as their metal complexes, were characterised using NMR and IR spectroscopy, and mass spectrometry. The molecular structure of the binuclear ruthenium(II) complex was determined by single-crystal X-ray diffraction analysis. The thiosemicarbazones and their complexes were evaluated for their in vitro antiplasmodial activities against the chloroquine-sensitive (NF54) and chloroquine-resistant (Dd2) Plasmodium falciparum strains, displaying activities in the low micromolar range. Selected compounds were screened for potential β-haematin inhibition activity, and it was found that two Rh(III) complexes exhibited moderate to good inhibition. Furthermore, the compounds were screened for their antitrichomonal activities against the G3 Trichomonas vaginalis strain, revealing a higher percentage of growth inhibition for the ruthenium and rhodium complexes over their corresponding ligand.
ISSN	14779226
Issue Number	5
Volume Number	44
e-ISSN	13645447
Journal	Dalton Trans.
Language	English
Publisher	Royal Society of Chemistry
Publisher Date	2015-02-07
Publisher Place	Great Britain (UK)
Access Restriction	Subscribed
Subject Keyword	Organometallic Compounds Chemistry Pharmacology Rhodium Ruthenium Silanes Thiosemicarbazones Animals Antineoplastic Agents Chemical Synthesis Toxicity Antiparasitic Agents CHO Cells Carbamates Cell Line, Tumor Cricetinae Cricetulus Hemeproteins Antagonists & Inhibitors Humans Hydrophobic And Hydrophilic Interactions Plasmodium Falciparum Drug Effects Structure-Activity Relationship Trichomonas Vaginalis Journal Article Research Support, Non-U.S. Gov't
Content Type	Text
Resource Type	Article
Subject	Inorganic Chemistry

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