Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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New Phenylaminopyrimidine (PAP) Anticancer Lead Compound with High Efficacy: Design, Synthesis, and in vitro Screening

  • El-Deeb, Ibrahim Mustafa (Life/Health Division, Korea Institute of Science and Technology) ;
  • Han, Dong-Keun (Life/Health Division, Korea Institute of Science and Technology) ;
  • Kim, In-Tae (Department of Chemistry, Kwangwoon University) ;
  • Lee, So-Ha (Life/Health Division, Korea Institute of Science and Technology)
  • Received : 2010.03.15
  • Accepted : 2010.05.03
  • Published : 2010.07.20
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Abstract

Phenylaminopyrimidines represent a large group of new selective anticancer agents, the majority of which exert their action through the inhibition of specific kinases. In this study, a new series of N-substituted-2-aminopyrimidines has been designed and synthesized. A selected group of the synthesized derivatives was screened at a single dose concentration of 10 ${\mu}M$ over a panel of 60 cancer cell-lines. Compound 12e has showed great inhibitory and strong lethal effect over almost all of the 60 cell-lines and accordingly was further tested in a 5-dose testing mode to determine its $IC_{50}$ values, where it showed great efficacies with intermediate potencies over the tested cell-lines. The compound was also tested over a panel of 52 kinases to explore its kinase inhibitory profile, and was found to be a selective but moderate inhibitor over FLT3 kinase.

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