Synthesis of Pyrazolo[3,4-d]pyrimidine Derivatives and Evaluation of their Src Kinase Inhibitory Activities
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Date
2013
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Publisher
ISCB
Abstract
A series of pyrazolo[3,4-d]pyrimidine derivatives was synthesized and evaluated for the Src kinase inhibitory activities. Compound 6e and 10c exhibited inhibition of Src kinase with an IC50 value of 5.6 and 5.1 μM, respectively. Hydroxamate derivative 15a was found to be a metal-mediated inhibitor for human Csk with an IC50 value of 2.0 μM showing 56-fold selectivity over Src kinase inhibition.
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Keywords
Chemistry, Synthesis, Anticancer agents, Pyrazolo[3,4-d]pyrimidine,