Biomedical Science Letters (대한의생명과학회지)

The Korean Society for Biomedical Laboratory Sciences (대한의생명과학회)
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Synthesis of 2-Thio-4-aminopyrimidine Derivatives as Anti-cancer Agent

  • Lee, Sang-Hyo (Department of Chemistry, College of Natural Sciences, Keimyung University) ;
  • Lee, Jin-Ho (Department of Chemistry, College of Natural Sciences, Keimyung University)
  • Published : 2009.06.30
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Abstract

The screening of the anti-cancer activity of the chemical library provided 2-thio-4-aminopyrimidine as the initial hit. The confirmation of structure and biological effect of hit was performed by synthesis and biological evaluation. The optimization of hit was performed by derivatization of substituents while keeping the core structure. The evaluation of growth inhibitory activity was carried out using SRB assay against 6 human cancer cell lines and human fibroblast. The growth inhibitory activity of compounds showed substituent dependency and more than 5 compounds showed complete growth inhibition of cancer cell lines at 10 ${\mu}M$ concentration. Chemical library screening followed by synthetic modification provided possibility that 2-thio-4-aminopyrimidine can be used as a new scaffold for the development of anti-cancer agent.

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