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http://dx.doi.org/10.5012/bkcs.2007.28.7.1114

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)
Publication Information
Bulletin of the Korean Chemical Society / v.28, no.7, 2007 , pp. 1114-1118 More about this Journal
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.
Keywords
Akt1 kinase; Inhibitory activity; Furo[2,3-d]pyrimidines;
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