International Journal of
Medicine and Medical Sciences

  • Abbreviation: Int. J. Med. Med. Sci.
  • Language: English
  • ISSN: 2006-9723
  • DOI: 10.5897/IJMMS
  • Start Year: 2009
  • Published Articles: 531

Full Length Research Paper

In vitro and in vivo antitumor activity of some synthesized 4-(2-pyridyl)-3-Thiosemicarbazides derivatives

Tarek A. Yousef
  • Tarek A. Yousef
  • Department of Chemistry, Faculty of Science, Mansoura University, Mansoura 35516, Egypt.
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Farid A. Badria
  • Farid A. Badria
  • Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura 35516 Egypt.
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Shabane E. Ghazy
  • Shabane E. Ghazy
  • Department of Chemistry, Faculty of Science, Mansoura University, Mansoura 35516, Egypt.
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Ola A. El-Gammal
  • Ola A. El-Gammal
  • Department of Chemistry, Faculty of Science, Mansoura University, Mansoura 35516, Egypt.
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Gaber M. Abu El-Reash
  • Gaber M. Abu El-Reash
  • Department of Chemistry, Faculty of Science, Mansoura University, Mansoura 35516, Egypt.
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  •  Accepted: 23 December 2010
  •  Published: 01 February 2011

Abstract

 

In search for potential antitumor drug candidates, a series of thiosemicarbazide derivatives were prepared via 4-(2-pyridyl)-3-thiosemicarbazide with phenyl isothiocyanate, benzoyl isothiocyanate, phenyl isocyanate and 4-pyridyl isothiocyanate. Effects of the synthesized compounds were tested using in vitro growth of a transplantable murine tumor cell line (Ehrlich Ascites Carcinoma) and in vivo-induced hepatocellular carcinoma (HCC) were studied. 1-(amino N-(pyridin-3yl)methanethiol-4-(pyridin-2-yl) thiosemicarbazide (H2PPY) has remarkably decreased the viable ascitic cell count as indicated by trypan blue dye exclusion assay. This compound prolonged the lifespan of Ehrlich Ascites Carcinoma (EAC) bearing-mice. Tumor inhibitory of this compound was demonstrated by significant improvement in blood picture (hemoglobin, RBC and WBC). The in vivo studies for H2PPY in HCC on rats showed a substantial improvement on both biochemical and histopathological parameters in comparison to non-treated HCC rats. The obtained data of the tested compound exhibited minimal adverse effects on the treated animals as compared to those of the untreated control groups.

 

Key words: Thiosemicarbazide derivatives, EAC, HCC, antitumor activity.