Exploring the Versatility of Cycloplatinated Thiosemicarbazones as Antitumor and Antiparasitic Agents
ORCID
Kirkwood M. Land: 0000-0001-5951-9630
Document Type
Article
Publication Title
Organometallics
Department
Biological Sciences
ISSN
0276-7333
Volume
31
Issue
16
DOI
10.1021/om300334z
First Page
5791
Last Page
5799
Publication Date
6-26-2012
Abstract
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 K2[PtCl4]. Two mononuclear (3 and 4) and two dinuclear (5 and 6) complexes were isolated upon cleavage of the Pt–Sbridging 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 β-hematin formation inhibition assays were also completed. Preliminary results suggest that ligand 1 and complex 3 do not hinder formation of β-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.
Recommended Citation
Chellan, P.,
Land, K. M.,
Shokar, A.,
Au, A.,
Hwan An, S.,
Clavel, C. M.,
Dyson, P. J.,
de Kock, C.,
Smith, P. J.,
Chibale, K.,
&
Smith, G. S.
(2012).
Exploring the Versatility of Cycloplatinated Thiosemicarbazones as Antitumor and Antiparasitic Agents.
Organometallics, 31(16), 5791–5799.
DOI: 10.1021/om300334z
https://scholarlycommons.pacific.edu/cop-facarticles/774
