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Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules

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2015
1793.pdf (1.001Mb)
Authors
Opsenica, Dejan
Radivojevic, Jelena
Matić, Ivana Z.
Štajner, Tijana
Knezevic-Usaj, Slavica
Djurkovic-Djakovic, Olgica
Šolaja, Bogdan
Article (Published version)
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Abstract
New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for their antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. The derivatives showed moderate, nM range antimalarial activities and low cytotoxicity. The N-phenylurea derivative 24 exhibited the best resistance indices (RIW2 = 0.44, RITM91C235 = 0.80) and was not toxic against human normal peripheral blood mononuclear cells (IC50 > 200 mu M). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukaemia K562 cells. One compound, derivative 21 with a primary amino group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another apicomplexan parasite. Subcutaneous administration at a dose of 10 mg kg(-1) day(-1) for 8 days allowed the survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment of ...apicomplexan parasites.

Keywords:
antimalarials / antiparasitic / peroxides / cancer / cytotoxicity
Source:
Journal of the Serbian Chemical Society, 2015, 80, 11, 1339-
Publisher:
  • Serbian Chemical Soc, Belgrade
Projects:
  • The synthesis of aminoquinoline-based antimalarials and botulinum neurotoxin A inhibitors (RS-172008)
  • Biological response modifiers in physiological and pathological conditions (RS-175011)

DOI: 10.2298/JSC150430063O

ISSN: 0352-5139

WoS: 000366585800001

Scopus: 2-s2.0-84957567719
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/1795
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IHTM

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