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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 28, Number 7
BKCSDE 28(7)
July 20, 2007 

Synthesis and Biological Evaluation of Furo[2,3-d]pyrimidines as Akt1 Kinase Inhibitors
Se Young Kim, Dong Jin Kim, Beom Seok Yang, Kyung Ho Yoo*
Akt1 kinase, Inhibitory activity, Furo[2,3-d]pyrimidines
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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