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.