Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Synthesis and Biological Evaluation of Furo[2,3-d]pyrimidines as Akt1 Kinase Inhibitors

  • Kim, Se-Young (Life Sciences Research Division, Korea Institute of Science and Technology) ;
  • Kim, Dong-Jin (Life Sciences Research Division, Korea Institute of Science and Technology) ;
  • Yang, Beom-Seok (Life Sciences Research Division, Korea Institute of Science and Technology) ;
  • Yoo, Kyung-Ho (Life Sciences Research Division, Korea Institute of Science and Technology)
  • Published : 2007.07.20
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Abstract

Based on the hit compound 4 derived from focused library, a series of furo[2,3-d]pyrimidines were designed, synthesized and evaluated for the inhibitory activity against Akt1 kinase. And their structure-activity relationships were investigated. Of these compounds, 3a having 2-thienyl and methyl groups at R1 and R2 showed the most potent activity with an IC50 value of 24 μ M. Introduction of the thienyl groups at C-5 and C- 6 positions significantly improved potency compared to furyl and phenyl groups.

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