Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
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Synthesis of 3-Alkylthio-6-Allylthiopyridazine Derivatives and Their Antihepatocarcinoma Activity

  • Kwon Soon-Kyoung (College of Pharmacy, Duksung Women's University) ;
  • Moon Aree (College of Pharmacy, Duksung Women's University)
  • Published : 2005.04.01
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Abstract

The allylthio group of allicin and other organosulfur compounds, isolated from garlic, is considered a pharmacophore, and a key structure component of the molecule, which affords biological activities. In the foregoing studies, various 3-alkoxy-6-allylthiopyridazine derivatives (K­compounds) were synthesized, and their biological activities tested in animals. As expected, the various derivatives showed good hepatoprotective activities on carbon tetrachloride-treated mice and aflatoxin B1-treated rats, and chemopreventive activities on hepatocarcinoma cells in rats. Other new pyridazine derivatives, with the oxygen atom at the 3-position of the 3-alkoxy­6-allylthiopyridazine displaced by sulfur (S), were synthesized, and their activities tested in vitro. Thio-K6, one of the sulfur-substituted compounds, showed better chemopreventive activity toward hepatocarcinoma cells.

Keywords

References

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