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  4. Exploring the Versatility of Cycloplatinated Thiosemicarbazones as Antitumor and Antiparasitic Agents
 
research article

Exploring the Versatility of Cycloplatinated Thiosemicarbazones as Antitumor and Antiparasitic Agents

Chellan, Prinessa
•
Land, Kirkwood M.
•
Shokar, Ajit
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2012
Organometallics

Tridentate cycloplatinated thiosemicarbazone complexes have been prepared from a biologically significant ligand, 3,4-dichloroacetophenone thiosemicarbazone (1). The tetranuclear complex 2 was prepared by reaction of the ligand with K-2[PtCl4]. Two mononuclear (3 and 4) and two dinuclear (5 and 6) complexes were isolated upon cleavage of the Pt-S-bridging bonds of the tetranuclear complex 2 with the appropriate phosphane ligand. Each complex was characterized using various analytical and spectroscopic techniques, and the molecular structures of 2-4 were also elucidated. The in vitro antiparasitic activities of these complexes against Plasmodium falciparum strains (D10 (chloroquine sensitive) and Dd2 (chloroquine resistant)) and Trichomonas vaginalis have been determined. Preliminary studies into their potential plasmodial target in the form of beta-hematin formation inhibition assays were also completed. Preliminary results suggest that ligand 1 and complex 3 do not hinder formation of beta-hematin. The antiproliferative activity of the complexes against the cisplatin-senstive A2780 and cisplatin-resistant A2780cisR human ovarian cancer cell lines has been evaluated. The complexes were found to exhibit moderate to weak inhibitory activities.

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Type
research article
DOI
10.1021/om300334z
Web of Science ID

WOS:000308263500013

Author(s)
Chellan, Prinessa
Land, Kirkwood M.
Shokar, Ajit
Au, Aaron
An, Seung Hwan
Clavel, Catherine M.  
Dyson, Paul Joseph  
De Kock, Carmen
Smith, Peter J.
Chibale, Kelly
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Date Issued

2012

Publisher

Amer Chemical Soc

Published in
Organometallics
Volume

31

Issue

16

Start page

5791

End page

5799

Editorial or Peer reviewed

REVIEWED

Written at

EPFL

EPFL units
LCOM  
Available on Infoscience
February 27, 2013
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/89647
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