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Synthesis and Antiproliferative Activity of Pyridinylcarbonylpyrimidines Against Melanoma Cell Line

  • Ahn, Hye-Mi (Life/Health Division, Korea Institute of Science and Technology) ;
  • Lee, Jun-A (Life/Health Division, Korea Institute of Science and Technology) ;
  • Kim, Hwan (Life/Health Division, Korea Institute of Science and Technology) ;
  • Oh, Chang-Hyun (Life/Health Division, Korea Institute of Science and Technology) ;
  • Lee, So-Ha (Life/Health Division, Korea Institute of Science and Technology) ;
  • Sim, Tae-Bo (Life/Health Division, Korea Institute of Science and Technology) ;
  • Hah, Jung-Mi (Department of Pharmacy, College of Pharmacy, Hanyang University) ;
  • Kim, Dong-Jin (Life/Health Division, Korea Institute of Science and Technology) ;
  • Yoo, Kyung-Ho (Life/Health Division, Korea Institute of Science and Technology)
  • Received : 2011.01.03
  • Accepted : 2011.02.07
  • Published : 2011.04.20

Abstract

The synthesis of the series of pyrimidinylamines 1a-d and pyrimidinylureas 1e-u bearing a novel pyridinylcarbonylpyrimidine scaffold and their antiproliferative activities against A375 human melanoma cell line were described. Among them, three compounds 1e, 1h, and 1o showed superior antiproliferative activities to Sorafenib ($IC_{50}=5.5{\mu}M$) as a reference compound. In our series, urea compound 1o having 4-chloro-3-trifluoromethyl moiety on the benzene nucleus exhibited very good antiproliferative activity with $IC_{50}$ value of $1.4{\mu}M$.

Keywords

References

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